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838 Cards in this Set
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|
* Time it takes for amt. of drug to fall to half of its value; this is a constant in first order kinetics
(majority of drugs) |
* Half-life
(t1/2) |
|
Relates the amount of drug in the body to the plasma concentration
|
Volume of distribution
(VD) |
|
Plasma concentration of a drug at a given time
|
Cp
|
|
The ratio of the rate of elimination of a drug to its plasma concentration
|
Clearance
(CL) |
|
The elimination of drug that occurs before it reaches systemic circulation
|
First pass effect
|
|
When the rate of drug input equals the rate of drug elimination
|
Steady State
|
|
* This step of metabolism makes a drug more hydrophilic and hence augments elimination
|
* Phase I
|
|
Different steps of Phase I
|
Oxidation
Reduction Hydrolysis |
|
* Inducers of P450
|
* Barbiturates
Phenytoin carbamazepine Rifampin |
|
* Inhibitors of P450
|
* Cimetidine
Ketoconazole Erythromycin Isoniazid Grapefruit |
|
Products of Phase II conjugation
|
Glucuronate
Acetic acid Glutathione sulfate |
|
Type of kinetics when a constant percentage of substrate is metabolized per unit time
|
First order kinetics
|
|
Drug elimination with a constant amount metabolized regardless of drug concentration
|
Zero order kinetics
|
|
Target plasma concentration times (Volume of distribution divided by boavailability)
|
Loading dose
(Cp*(Vd/F)) |
|
Concentration in the plasma times (clearance divided by bioavailability)
|
Maintenance dose
(Cp*(CL/F)) |
|
Strength of interaction between drug and its receptor
|
Affinity
|
|
Selectivity of a drug for its receptor
|
Specificity
|
|
Amount of drug necessary to elicit a biological effect
|
Potency
|
|
* Ability of drug to produce a biologic effect
|
* Efficacy
|
|
Ability of a drug to produce 100% of the maximum response regardless of the potency
|
Full agonist
|
|
Ability to produce less than 100% of the response
|
Partial Agonist
|
|
Ability to bind reversibly to the same site as the drug and without activating the effector system
|
Competitive Antagonist
|
|
Class of drugs wtih ability to decrease the maximal repsonse to an agonist
|
Noncompetetive antagonist
|
|
* A hormone whose MOA utilizes intracellular receptors
|
* Thyroid and steroid hormones
|
|
* A hormone whose MOA utilizes transmembrane receptors
|
* Insulin
|
|
Class of drugs whose MOA utilizes ligand gated ion channels
|
Benzodiazepines and calcium channel blockers
|
|
Median effective dose required for an effect in 50% of the population
|
ED50
|
|
Median toxic dose required for a toxic effects 50% of the population
|
TD50
|
|
Dose which is lethal to 50% of the population
|
LD50
|
|
Window between therapeutic effect and toxic effect
|
Therapeutic index
|
|
Term for a high margin of safety
|
High therapeutic index
|
|
Term for a narrow margin of safety
|
Low therapeutic index
|
|
Antidote used for Lead poisoning
|
Dimercaprol, EDTA
|
|
Antidote used for cyanide poisoning
|
Nitrites
|
|
Antidote used for anticholinergic poisoning
|
Physostigmine
|
|
** Antidote used for organophosphate/anticholinesterase poisoning
|
** Atropine, pralidoxime (2-PAM)
|
|
Antidote used for iron salt toxicity
|
Deferoxamine
|
|
* Antidote used for acetaminophen (APAP) toxicity
|
* N-acetylcysteine
(Mucomyst) |
|
Antidote for Arsenic, Mercury, Lead, & Gold poisoning
|
Dimercaprol
|
|
Antidote used in poisoning:
Copper (Wilson's disease) Lead Mercury Arsenic |
Penicillamine
|
|
** Antidote used for Heparin overdose
|
** Protamine
|
|
* Antidote used for warfarin toxicity
|
* Vitamin K & Fresh Frozen Plasma (FFP)
|
|
** Antidotes for t-PA, streptokinase
|
** Aminocaproic acid
|
|
Antidote used for methanol and ethylene glycol
|
Ethanol or fomepizole
|
|
* Antidote used for opiod toxicity
|
* Naloxone (iv)
Naltrexone (po) |
|
* Antidote used for benzodiazepine
|
* Flumazenil
|
|
Antidote used for TCA's
|
Sodium bicarbonate
|
|
Antidote used for Carbon monoxide poisoning
|
100% O2 and Hyperbaric O2
|
|
Antidote used for digitalis toxicity
|
Digibind
(also need d/c digoxin, normalize K+, and Lidocaine if pt is arrhythmic) |
|
The Fraction of administered dose of a drug that reaches systemic circulation
|
Biovailability
(F) |
|
Antidote used for beta agonist toxicity
(e.g. Metaproterenol) |
Esmolol
|
|
Antidote for methotrexate toxicity
|
Leucovorin
|
|
Antidote for beta-blocker and hpoglycemia
|
Glucagon
|
|
Antidote useful for some drug induced Torsades de pointes
|
Magnesium Sulfate
|
|
Antidote for hyperkalemia
|
Sodium polystyrene sulfonate
(Kayexalate) |
|
Antidote for salicylate intoxication
|
Alkalinize the urine, dialysis
|
|
Constant proportion of cell population killed rather than a constant number
|
Log-kill hypothesis
|
|
Treatment w/cancer chemotherapy at high doses every 3-4 weeks, too toxic to be used continuously
|
Pulse Therapy
|
|
Toxic effect of anticancer drug can be lessened by rescue agents
|
Rescue Therapy
|
|
Drug used concurrently with toxic anticancer agents to reduce renal precipitation of urates
|
Allopurinol
|
|
Pyrimidine analog that causes "Thymine-less death" given with leucovorin rescue
|
5-Fluoracil (5-FU)
|
|
Drug used in cancer therapy causes Cushing-like symptoms
|
Prednisone
|
|
Side effect of Mitomycin
|
SEVERE myelosuppression
|
|
MOA of cisplatin
|
Alkylating Agent
|
|
Common toxicities of cisplatin
|
Nephro and Ototoxicity
|
|
Analog of hypoxanthine, needs HGPRTase for activation
|
6-mercaptopurine (6-MP)
|
|
** Interaction with this drug requires dose reduction of 6-MP
|
** Allopurinol
|
|
* May protect against doxorubicin toxicity by scavenging free radicals
|
* Dexrazoxane
|
|
* Blows DNA (Breaks DNA strands), limiting SE is pulmonoary fibrosis
|
* Bleomycin
|
|
Bleomycin
Vinblastin Etoposide Cisplatin Produce almost 100% response when all agents are used for this neoplasm |
Testicular Cancer
|
|
ABVD regimen used or HD, but appears less likely to cause sterility and secondary malignancies thatn MOPP
|
Adriamycin (doxorubicin)
Bleomycin Vinblastin Dacarbazine |
|
Regimen used non-Hodgkin's lymphoma
|
CHOP + Rituximab
Cyclophosphamide Doxorubicin Vincristine Prednisone +++ Rituximab |
|
Regimen used for breast cancer
|
CMF + Tamoxiphen if ER+
Cyclophosphamide Methotrexate Fluorouracil |
|
Alkylating agent, vesicant that causes tissue damage with extravasation
|
Mechlorethamine
|
|
Anticancer drug also used in RA, produces acrolein in urine that leads to HEMORRHAGIC CYSTITIS
|
Cyclophosphamide
|
|
Prevention of cyclophosphamide induced hemorrhagic cystitis
|
Hydration and MESNA (mercaptothanesulfonate)
|
|
Microtubule inhibitor that causes peripheral neuropathy, foot drop (e.g. ataxia) and "pins and needles" sensation
|
Vincristine
|
|
** Interaction with microtubules (but unlike vinca which prevent disassembly of tubules) it stabilizes tubilin and cells remain frozen in metaphase
|
** Paclitaxel (taxol)
|
|
Toxicities include nephrotoxicity and ototoxiity, leadin to a severe interaction with aminoglycosides
|
Cisplatin
|
|
Agent similar to cisplatin, less nephrotoxic, but greater myelosuppression
|
Carboplatin
|
|
Converts asparagine to aspartate and ammonia, denies cancer cells of essential AA (asparagine)
|
L-asparaginase
|
|
Used for Hairy cell leukemia; it stimulates NK cells
|
Interferon alpha
|
|
Anti-androgen used for prostate cancer
|
Flutamide (Eulexin)
|
|
** Anti-estrogen used for estrogen receptor + breast cancer
|
** Tamoxifen
|
|
Aromatase inhibitor used in breast cancer
|
Letrozole
Anastrozole |
|
Newer estrogen receptor antagonist used in advanced breast cancer
|
Toremifene
(Fareston) |
|
Some cell cycle specific anti-cancer drugs
|
Bleomyin, vinca alkaloids, antimetabolites (5-FU, 6-MP, methotrexate, etoposide)
|
|
Some cell cycle non-specific drugs
|
Alkylating agents (mechlorethamine, cyclohosphamide), antibiotics (doxorubicin, daunorubicin) cisplatin, nitrosourea
|
|
* Anti-emetics used in association with anti-cancer drugs that are 5-HT3 (serotonin receptor subtype) antagonists
|
* Odansetron
Gransetron |
|
Nitrosoureas with high lipophilicity, used for brain tumors
|
Carmustine (BCNU)
& Lomustine (CCNU) |
|
Produces disulfiram-like reaction with ethanol
|
Procarbazine
|
|
Somatostatin (SRIF) analog used for acromegaly, carcinoid, glucagonoma, and other GH producing pituitary tumors
|
Ocreotide
|
|
Somatotropin (GH) analog used in GH deficiency (dwarfism)
|
Somatrem
|
|
GHRH analog used as a diagnostic agent
|
Sermorelin
|
|
GnRH agonist used for infertility or different types CA depending on pulsatile or steady usage respectively
|
Leuprolide
|
|
GnRH antagonist wtih more immediate effects, used for infertility
|
Ganirelix
|
|
* Dopamine agonist (or Parkinson's disease) used also for hyperprolactinemia
|
* Bromocriptine
|
|
* Hormone inhibiting prolactin release
|
* Dopamine
|
|
** ACTH analog used or diagnosis of pt's with corticosteroid abnormality
|
** Cosyntropin
|
|
* Synthetic analog of ADH hormone used for diabetes insipidus and nocturnal enuresis
|
* Desmopressin (DDVAP)
|
|
** SE of OC's
|
** Increased thromboembolic events
|
|
** Most widely used thyroid drugs such as Synthroid and Levoxyl contain
|
** L-thyroxine (T4)
|
|
T3 compound less widely used
|
Cytomel
|
|
Anti-thyroid drugs
|
Thioamides
Iodides Radioactive Iodine Ipodate |
|
Thioamide agents used in hyperthyroidism
|
Methimazole nd propylthiouracil (PTU)
|
|
* Thioamide less likely to cross placenta, inhibits peripheral conversion of T4 to T3 in high doses and should be used with extreme caution in pregnancy
|
* PTU
|
|
* PTU (propylthiouracil) MOA
|
* Inhibits thyroid hormone synthesis by blocking iodination of the tyrosine residues of thyroglobulin
|
|
Can be effective for "short term therapy" of thyroid storm, but after several weeks of therapy causes an exacerbation of hyperthyroidism
|
Iodide salts
|
|
** Dose may need to be increased during pregnancy or with OC's due to increased TBG in plasma
|
** Thyroxine
|
|
Permanently cures thyrotoxicosis, patients will need thyroid replacement therapy thereafter. Contraindicated in pregnancy
|
Radioactive iodine
|
|
Radio contrast media that inhibits the conversion of T4 to T3
|
Ipodate
|
|
Block cardiac adverse effects of thyrotoxicosis such as tachycardia, inhibits the conversion of T4 to T3
|
Beta-blockers such as propranolol
|
|
Vitamins containing iron should NOT be taken simultaneously with levothyroxine because....
|
Iron deiodinates thyroxine
|
|
Thyroxine dose may need to be increased in hypothyroid patient during pregnancy because
|
Estrogens increase maternal TBG
|
|
3 zones of adrenal cortex and their products
|
Glomerulosa (mineralocorticoids)
fasciculata (glucocorticoid=GD) Reticularis (adrenal androgens) |
|
Mneumonic for 3 zones of adrenal cortex
|
GFR
Go Find Rex Make Good ex |
|
Used for addison's disease, congenital adrenal hyperplasia (CAH), inflammation, allergies, and asthma (as local inhalation)
|
Glucocorticoids
|
|
Short acting glucocorticoids
|
Cortisone & Hydroxycortisone
(equivalent to cortisol) |
|
Intermediate acting glucocorticoids
|
Prednisone
Methylprednisolone Prednisolone & Triamcinolone |
|
Long acting glucocorticoids
|
Betamethasone & Dexamethasone
|
|
Mineralocorticoids
|
Fludrocortisone & deoxycorticosterone
|
|
* Some side effects of corticosteroids
|
* Osteopenia
impaired wound healing inc. risk of infection inc. appetite HTN edema PUD Euphoria psychosis stria thinning of skin |
|
Period of time of therapy after which GC therapy will need to be tapered
|
5-7- days
|
|
Used for Cushing's syndrome
(increased corticosteroid) |
Dexamethasone suppression test
|
|
Inhibits conversion of cholesterol to pregnenolone therefore inhibiting corticosterol synthesis
|
Aminoglutethimide
|
|
Antifungal agent used for inhibition of all gonadal and adrenal steroids
|
Ketoconazole
|
|
Antiprogestin used as potent antagonist of GC receptor
|
Mifepristone
|
|
* Diuretic used to antagonize aldosterone receptors
|
* Spironolactone
|
|
** Common SE of spironolactone
|
** Gynecomastia and HYPERkalemia
|
|
Slightly increased risk of breast cancer, endometrial cancer, heart disease (questionable) has beneficial effects on bone loss
|
Estrogen
|
|
Antiestrogen drugs used for fertility and breast cancer respectively
|
Clomiphene and tamoxifen
|
|
Common SE of tamoxifen and raloxfene
|
Hot flashes
|
|
** Selective estrogen receptor modulator (SERM) used for prevention of osteoporosis and prophylaxis in women with risk factors for breast cancer
|
** Raloxifene
|
|
* Non-steroidal estrogen agonist causes clear cell adenocarcinoma of the vagina in daughters of women who used it during pregnancy
|
* Diethylstilbestrol (DES)
|
|
Estrogen mostly used in oral contraceptives (OC)
|
Ethinyl estradiol and mestranol
|
|
Anti-progesterone used as abortifacient
|
Mifepristone (RU-486)
|
|
Constant low dose of estrogen and increasing dose of progestin for 21 days (last 5 days are sugar pills or iron prep)
|
Combination oral contraceptives (OC)
|
|
Oral contraceptive available in transdermal patch
|
Ortho-Evra
|
|
* Converted to more active form DHT by 5 alpha-reductase
|
* Testosterone
|
|
5 alpha-reductase inhibitor used for benign prostatic hyperplasia (BPH) and male pattern baldness
|
Finasteride (Proscar and Propecia respectively)
|
|
Anabolic steroid that has potential for abuse
|
Nandrolone
Oxymetholone & Oxandrolone |
|
Anti-androgen used for HIRSUTISM in females
|
Cyproterone acetate
|
|
** Drug is used with testosterone for male fertility
|
** Leuprolide
|
|
What do alpha cells in the pancreas produce?
|
Glucagon
|
|
What do beta cells in the pancreas produce?
|
Insulin
|
|
Where are beta cells found in the pancreas?
|
Islets of Langerhans
|
|
What do delta cells in the pancreas produce?
|
Somatostatin
|
|
* Product of proinsulin cleavage used to asses insulin abuse
|
* C-peptide
|
|
* Exogenous insulin contains
|
* little C-peptide
|
|
Endogenous insulin contains
|
Normal C-peptide
|
|
Very rapid acting insulin, having fastest onset and shortest duration of action
|
Lispro (Humalog)
Aspart Glulisine |
|
Rapid acting, crystalline zinc insulin used to reverse acute hyperglycemia
|
Regular (Humulin R)
|
|
* Long acting insulin
|
* Ultralente (Humulin U)
|
|
Ultra long acting insulin, has over day duration of action
|
Glargine (Lantus), detemir
|
|
Major SE of insulin
|
Hypoglycemia
|
|
Important in synthesis of glucose to glycogen in the LIVER
(Insulin dependent) |
GLUT 2
|
|
Important in MUSCLE and ADIPOSE tissue for glucose transport across muscles and TG storage by lipoprotein lipase activation
|
GLUT 4
|
|
Examples of alpha-glucosidation inhibitors (AGI's)
|
Acarbose, miglitol
|
|
MOA of AGI's
|
Act on intestine, delay digestion and absorption of glucose formed from diestion of starch and disaccarides
|
|
SE of AGI's
|
Flatulence (do not use beano to tx), diarrhea, abdominal cramps
|
|
Alpha-glucosidase inibitor assoc. with elevation of LFT's
|
Acarbose
|
|
* Amino acid derivative, active as an insulin secretagogue
|
* Nateglinide
|
|
MOA of nateglinide
|
Insulin secretagogue - closes ATP-sensitive K+ channel
|
|
Biguanide
|
Metformin
|
|
Drugs available in combination with metformin
|
Glyburide
Glipizide Rosiglitazone |
|
MOA of Metformin
|
Decreases hepatic glucose production and intestinal glucose absorption; increase insulin sensitivity
|
|
Vascular effects of metformin
|
Decreased micro and macro vascular disease
|
|
Most important potential SE of metformin
|
Lactic acidosis
|
|
Incidence of hypoglycemia with metformin
|
NONE
|
|
Meglitinide class of drugs
|
Repaglinide
|
|
MOA of repaglinide
|
Insulin release from pancreas;
Faster and sorter acting than sulfonylurea |
|
First generation sulfonlurea
|
Chlorpropamide
tolbutamide tolazamide, etc. |
|
Second generation sulfonylurea
|
Glyburide
Glipizide Glimepiride, etc. |
|
MOA of both generations
|
Insulin release from pancreas by modifying K+ channels
|
|
Common SE of sulfonylureas, repaglinide, and nateglinide
|
Hypoglycemia
|
|
Sulfonylurea NOT recommended for elderly because of very long half life
|
Chlorpropamide
|
|
Thiazolidinediones
|
Pioglitazone
Rosiglitazone Troglitazone (withdrawn from market) |
|
Reason troglitazone was withdrawn from market
|
Hepatic toxicity
|
|
MOA of thiazolidinediones
|
Stimulate PPAR-gamma receptor to regulate CHO and lipid metabolism
|
|
SE of thiazolidinediones
|
Edema + Anemia
Interaction with drugs that undergo CYP450 3A4 metabolism |
|
Hyperglycemia agent that increase cAMP and results in glycogenolyis, gluconeogenesis, reverses hypoglycemia, also used to reverse severe beta-blcker overdose adn smooth muscle relaxation
|
Glucagon
|
|
Available bisphosphonates
|
Alendronate
Etidronate Risedronate Pamidronate Tiudornate Zoledronic acid |
|
MOA of bisphosphonates
|
Inhibits osteoCLAST bone resorption
|
|
Only bisphosphonate available IV
|
Etidronate
|
|
Uses of bisphosphonates
|
Osteoporosis
Paget's disease Osteolytic bone lesions Hypercalcemia from malignancy |
|
Major SE of bisphosphonates
|
Chemical esophagitis
|
|
Bisphosphonate that cannot be used on continuous basis b/c it causes OSTEOMALACIA
|
Etidronate
|
|
Used for prevention of postmenopausal osteoporosis in women
|
Estrogen (HRT)
|
|
** Increase bone density, also being tested for Breast cancer prophylaxis
|
** Raloxifene (SERM)
|
|
* Used intranasally and decreases bone resorption
|
* Calcitonin (salmon prep)
|
|
Used especially in postmenopausal women, dosage should be 1500mg
|
Calcium
|
|
Vitamin given with Calcium to ensure proper absorption
|
Vitamin D
|
|
Disease caused by excess ergot alkaloids
|
St. Anthony's Fire
|
|
Endogenous substance commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides
|
Autocoids
|
|
Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is assoc. with severe peptic ulceration and diarrhea
|
Zollinger-Ellison Syndrome
|
|
* Drug that causes contraction of the uterus
|
* Oxytocin
|
|
* Distribution of Histamine receptors H1, H2, and H3
|
* H1: Smooth muscle
H2: stomach, heart, and mast cells H3: nerve endings, CNS respectively |
|
* Prototype antagonist fo HI and H2 receptors
|
* Diphenhydramine and cimetridine, respectively
|
|
** 1st generation antihistamine that is highly sedating
|
** Diphenhydramine
|
|
1st generation antihistamine that is least sedating
|
Chlorpheniramine or cyclizine
|
|
* 2nd generation antihistimines
|
* Fexofenadine
Loratidine Cetirizine |
|
Generation of antihistamine that has the MOST CNS effects
|
First generation due to being more lipid-soluble
|
|
Major indication for H1 receptor antagonist
|
Use in IgE mediated allergic reation
|
|
Antihistamine that can be used for anxiety and insomnia and is not addictive
|
hydroxyzine (Atarax)
|
|
H1 antagonist used in motion sickness
|
Dimenhydrinate
Meclizine and other 1st gen's |
|
MC SE of 1st generation anihistamines
|
Sedation
|
|
Lethal arrhythmias resulting from concurrent therapy with azole fungals (metabolized by CYP 3A4) and these antihistamines which inhibit he 3A4 isoenzyme
|
Terfenadine and astemizole
(have been removed from the market) |
|
* H2 blocker that causes the most interactions with other drug
|
* Cimetidine
|
|
Clinical use for H2 blockers
|
Acid reflux disease
Duodenal ulcer Peptic Ulcer disease |
|
Receptors for Serotonin (5HT-1) are located
|
Mostly in the brain and they mediate synaptic inhibition via increased K+ conductance
|
|
** 5HT-1d agonist used for migraine headaches
|
** Sumatriptan
Naratriptan & Rizatriptan |
|
Triptan available in parenteral and nasal formulation
|
Sumatriptan
|
|
H1 blocker that his also a serotonin antagonist
|
Cyproheptadine
|
|
** Agents for redution of postpartum bleeding
|
** Oxytocin, ergonovine and ergotamine
|
|
** Agents used in treatment of carcinoid tumor
|
** Ketanserin cyproheptadine, and phenoxybenzamine
|
|
*** 5HT-3 antagonist used in chemotherapeutic induced emesis
|
*** Odansetron
Granisetron Dolasetron Alosetron |
|
5HT-3 antagonist that has been associated with QRS and QTc proongation and should not be used in patient wiht HEART disease
|
Dolasetron
|
|
** DOC to treat chemo-induced nausea and vomiting
|
** Odansetron
|
|
Drug used in ergot-alkaloids overdose, ischemia and gangrene
|
Nitroprusside
|
|
Reason ergot alkaloids are contraindicated in Pregnancy
|
Uterine contraction
|
|
SE of ergt alkaloids
|
Hallucinations resembling psychosis
|
|
* Ergot alkaloid used as an illicit drug
|
* LSD
|
|
* Dopamine agonist used in hyperprolactinemia
|
* Bromocriptine
|
|
Peptide causing increased capillary permeability and edema
|
Bradykinin & histamine
|
|
* Mediator of tissue pain, edema, inactivated by ACE, and maybe a contributing factor to the development of angioedema
|
* Bradykinin
|
|
* Drug causing depletion of Substance P (vasodilator)
|
* Capsaicin
|
|
* Prostaglandins that cause abortions
|
* Prostaglandin E1 (misopristol)
PGE2, an PGF-alpha |
|
Difference between COX 1 and COX 2
|
COX 1 is found throughout the body and COX 2 is only found in inflammed tissue
|
|
Drug that selectively inhibits COX 2
|
Celecoxib & rofecoxib
|
|
* Inhibitor of lipoxygenase
|
* Zileuton
|
|
Major SE of Zileuton
|
Liver toxicity
|
|
Inhibitor of Lekotrienes (LTD4) receptors and used in asthma
|
Zafirlukast and montelukast
|
|
* Used in pediatrics to maintain patency of Ductus Arteriosis
|
* PGE1
|
|
Approved for used in severe pulmonary HTN
|
PGI2 (epoprostenol)
|
|
* Prostaglandin used in the treatment of impotence
|
* Alprostadil
|
|
Irreversible, non-selective COX inhibitor
|
Aspirin
|
|
Class of drugs that reversibly inhibit COX
|
NSAIDS
|
|
Primary endogenous substrate for Nitric Oxidase Synthase
|
Arginine
|
|
* MOA and effect of Nitric oxide
|
* Stimulates cGMP which leads to vascular smooth muscle relaxation
|
|
Long acting beta 2 agonist used in asthma
|
Salmeterol
|
|
* Muscarinic antagonist used in asthma
|
* Ipratropium
|
|
* MOA of cromolyn
|
* Mast cell stabilizer
|
|
Methylxanthine derivative used as a remedy for intermittent claudication
|
Pentoxifylline
|
|
MOA of corticosteroids
|
Inhibit phospholipase A2
|
|
* SE of longterm (>5days) corticosteroid therapy and remedy
|
* Adrenal suppression and weaning slowly, respectively
|
|
** MOA of quinolones
|
** Inhibit DNA gyrase
|
|
MOA of penicillin
|
Block cell wall synthesis by inhibiting peptidoglycan cross-linkage
|
|
* Drug used for MRSA
|
* Vancomycin
|
|
** Vancomycin MOA
|
** Blocks peptidoglycan synthesis
|
|
Type of resistance found with vancomycin
|
Point mutation
|
|
* Meningitis prophylaxis in exposed patients
|
* Rifampin
|
|
* Technique used to diagnose perianal itching, and the drug used to treat it
|
Scotch tape technique
& MeBENDazole |
|
Two toxicities of aminoglycosies
|
Nephro and Ototoxicity
|
|
DOC for Legionnaire's disease
|
Erythromycin
|
|
* MOA of Sulfonamides
|
* Inhibit dihydropteroate synthase
|
|
Penicillins active agaist penicillinase secreting bacteria
|
Methicillin, nafcillin, & dicloxacillin
|
|
*** Cheap wide spectrum antibiotic DOC for otitis media
|
*** Amoxicillin
|
|
Class of antibiotics that have 10% cross sensitivity with penicillins
|
Cephalosporins
|
|
PCN active against pseudomonas
|
Carbenicillin
Piperacillin Ticarcillin |
|
Antibiotic causing Red Man Syndrome, and Prevention
|
Vancomycin
Infuse at a slow rate and antihistamines |
|
Drug causes teeth discoloratoin
|
Tetracyclines
|
|
MOA of tetracyclyine
|
Decreases protein synthesis by inhibiting 30S ribosome
|
|
Drug that causes gray baby syndrome and aplastic anemia
|
Chloramphenicol
|
|
Drug notorious for causing pseudomembranous colitis
|
Clindamycin
|
|
** DOC for tx of pseudomembranous colitis
|
** Metronidazole
|
|
Treatment of resistant pseudomembranous colitis
|
ORAL vancomycin
|
|
* Anemia caused by Timethoprim
|
* Megaloblastic anemia
|
|
Reason fluoroquinolones are C/I in children and pregnancy
|
Cartilage damage
|
|
* DOC for Giardia, bacterial vaginosis, pseudomembranous colitis, and trichomonas
|
* Metronidazole
|
|
* Treatment of TB patient
|
* Rifampin
Isoniazid Pyrazinamide Ethambutol |
|
Metronidazole SE if givenwith alohol
|
Disulfiram-like reaction
|
|
* Common SE Rifampin
|
* Red Urine discoloration
|
|
MOA of nystatin
|
Bind ergosterol in fungal cell membrane
|
|
Neurotoxicity with Isoniazid (INH) is prevented by
|
B6 (Pyridoxine)
|
|
Toxicity of amphotericin
|
Nephrotoxicity
|
|
SE seen onlyin men with administration of Ketoconazole
|
Gynecomastia
|
|
Topical DOC in impetigo
|
Topical mupirocin
(Bactroban) |
|
* DOC for influenza A
|
* Amantadine
|
|
* DOC for RSV
|
* Ribavarin
|
|
DOC for CMV retinitis
|
Ganciclovir
Think of Eez-E and his CMV retinitis from HIV, Gang-ciclovir |
|
SE for ganciclovir
|
Neutro, leuko and Thrombocytopenia
|
|
Anti-viral agents associated with Stephen Johnson syndrome
|
Nevirapine
Amprenavir Stephen Johnson would Never rape and-pre-y on girls |
|
* HIV anti-viral class known to have severe drug interactions by causing inbihition of metabolism
|
* Protease inhibitors
|
|
Antivirals that are teratogens
|
Delavirdine
Efavirenz & Ribavarin |
|
Antivirals associated with neutropenia
|
Ganciclovir
Zidovudine Saquinavir Interferon |
|
HIV med used to reduce transmission during birth
|
AZT (zidovudine)
|
|
Drug used for African sleeping sickess
|
Suramin
|
|
Drug used in Chagas disease
|
Nifurtimox
|
|
Cephalosporins able to cross to BBB
|
Cefuroxine (2nd gen) &
Cefixime (3rd gen) |
|
* Drug used for N. gonnorrhea in females
|
* Ceftriaxone
|
|
Cephalosporin causes kernicterus in neonates
|
Ceftriaxone or cefuroxime
|
|
SE of INH
|
Peripheral neuritis and hepatitis
|
|
Aminoglycoside that is least ototoxic
|
Streptomycin
|
|
Drug used in exoerythrocytic cycle of malaria
|
Primaquine
|
|
Oral antibiotic of choice of moderate inflammatory acne
|
Minocycline
|
|
DOC for LEPROSY
|
Dapsone, Rifampin & Clofazimine combo
|
|
* DOC for Herpes and its MOA
|
* Acyclovir; incorporated intoviral DNA and chain termination
|
|
* Anti-microbials that cause hemolysis in G6Pd-deficient patients
|
* Sulfonamides
|
|
MOA of erythromycin
|
Inhibition of protein synthesis at the 50s subunit of ribosome
|
|
* Antibiotic frequently used for chronic UTI prophylaxis
|
* TMP/SMX
|
|
Lactam that can be used in PCN allergic pts
|
Aztreonam
|
|
SE of Imipenem
|
Seizures
|
|
Anti-viral with a dose limiting toxicity of PANCREATITIS
|
Didanosine
|
|
Common side effect of hypnotic agents
|
Sedation
|
|
Occurs when sedative hypnotics are used chronically or at high doses
|
Tolerance
|
|
The MC type of drug interaction of sedative hypotics with other depressant medications
|
Additive CNS depression
|
|
Benzodiazepines used to promote Sleep
|
Temazpam
Trizolam Flurazepam |
|
Benzo used for Anxiety
|
Alpazolam
|
|
Non-benzodiaepine used as an anxiolytic
|
Buspirone
|
|
Non-benzo used for Sleep
|
Zolpidem
|
|
* Major effect of benzo's on sleep at high doses
|
* REM is decreased
|
|
Neurologic SE of benzo's
|
Anterograde amnesia
|
|
* Reason benzo's are used cautiously in pregnancy
|
* Ability to cross the placenta
|
|
Main route of metaolism for benzo's
|
Hepatic
|
|
Benzo that undergo's extrahepatic conjugation (which are usefulin older or hepatically impaired)
|
Lorazepam
Oxazepam Temazepam |
|
MOA for benzo's
|
increase teh FREQUENCY of GABA-mediated chloride ion channel opening
|
|
* Antidote to benzo overdose (antagonist that reverses teh CNS effects)
|
* FLumazenil
|
|
Benzo with useful relaxant effects in skeletal muscle spasticity of central origin
|
Diazepam
|
|
Benzo that has efficacy against absence seizures and in anxiety states such as AGORAPHOBIA
|
Clonazepam
|
|
Benzo's that are the most effective in t tx of panic disorder
|
Aprazolam and Clonasepam
|
|
Benzodiazepine that is used for anesthesia
|
Midazolam
|
|
DOC for status spilepticus
|
Diazepam
|
|
Longer acting benzo's used in the management of withdrawal staes of ALCOHOL and other drugs
|
Chlordiazepoxide & Diazepam
|
|
Agents having active metabolites, long half lives, and a high incidence of adverse effects
|
Diazepam
Flurazepam Chlordiazepoxide & Clorazepate |
|
Barbiturates may precipitate this hematologic condition
|
Acute intermittent porphyria
|
|
Barbiturates decrease the effectiveness of many other drugs via this pharmacokinetics property
|
Liver enzyme INDUCTION
|
|
Barbiturates MOA
|
Increase the DURATION of GABA mediated chloride ion channels
|
|
Barbiturate used for the induction of Anesthesia
|
Thiopental
|
|
Site of action for zaleplon and zolpidem
|
Benzodiazepine receptor BBZ1
(although do not have a benzodiazepine ring structure) |
|
Good hypnotic activity w/ less CNS SE than most benzo's
|
Zolpidem
Zaleplon |
|
Agent that is a partial agonist for the 5-Ht1A receptor
|
Buspirone
|
|
DOC for generalized anxiety disorder, NOT effective in Acute Anxiety!
|
Buspirone
|
|
* Agent that is metabolized to acetaldehyde by alcohol dehydrogenase and microsomal ethanol-oxidizing system (MEOS)
|
* Ethanol
|
|
Agent with zero-order kinetics
|
Phenytoin
Ethanol Aspirin in high toxic doses |
|
Rate limiting step of alcohol metabolism
|
Aldehyde dehydrogenase
|
|
* System that increases in activity with chronic ethanol exposure and may contribute to tolerance
|
* MEOS
|
|
Enzyme that metabolizes acetaldehyde to acetate
|
Aldehyde dehydrogenase
|
|
Agents that inhibit alcohol dehydrogenase
|
Disulfiram
Metronidazole Certain sulfonylureas and cephalosporins |
|
Agent used in the treatment of alcoholism, if alcohol is consumed concurrently, acetaldehyde builds up and results in nausea, headache, flushing and hypotension
|
Disulfiram
|
|
* The MC neurologic abnorm. in Chronic Aloholics
|
* Peripheral neuropathy (also excessive alcohol use is assoc. with HTN, anemia & MI)
|
|
Agent that is a teratogen and causes fetal alcohol syndrome
|
Ethanol
|
|
Agent that is the antidote for methanol overdose
|
Ethanol, fomepizole
|
|
Drug that inhibits alcohol dehydrogenase adn is used in ethylene glycol exposure
|
Fomepizole
|
|
Most frequent route of metabolism
|
Hepatic enzymes
|
|
MOA for Phenytoin, Carbamazepine, Lamotrigine
|
Sodium channel blockade
|
|
MOA for Benzo's and barbiturates
|
GABA-related targets
|
|
MOA for Ethosuximide
|
Ca channels
|
|
MOA for Valproic acid at high doses
|
Affect Ca, K, and Na channels
|
|
* DOC for generalized tonic-clonic and partial seizures
|
* Valproic acid and Phenytoin
|
|
DOC for Febrile Seizures
|
Phenobarbital
|
|
* DOC's for absence seizures
|
* Ethosuximide & Valproic acid
|
|
* DOC for myoclonic seizures
|
* Valproic acid
|
|
DOC's for for status epilepticus
|
i.v. Diasepam for short term (acute) treatment; phenytoin for prolonged therapy
|
|
Drugs that can be used for infantile spasms
|
Corticosteroids
|
|
Anti-seizure drugs used also for bipolar affective disorder (BAD)
|
Valproic acid, carbamazepine, phenytoin and gabapentin
|
|
Anti-seizure drugs used for Trigeminal Neuralgia
|
Carbamazepine
|
|
* Anti-seizure drugs used also for pain of neuropathic origin
|
* Gabapentin
|
|
Anti-seizure agent that exhibits non-linear metabolism, highly protein bound, causes Fetal hydantoin syndrome and stimulates hepatic metabolism
|
Phenytoin
|
|
* SE of phenytoin
|
* Gingival hyperplasia
hirsutism nystagmus diploplia and ataxia SLE-like syndrome megaloblastic anemia (decr. folate absorption) |
|
Anti-seizure that induces formation of liver drug-metabolism enzymes, is teratogen and can cause craniofascial anomalies and spina bifida
|
Carbamazepine
|
|
Agent that inhibits hepatic metabolism, is hepatotoxic and teratogen that can cause neural tube defects and gastrointestinal distress
|
Valproic acid
|
|
Labratory value required to be monitored for patients on valproic acid
|
Serum ammonia and LFT's
|
|
SE for Lamotrigine
|
Stevens-Johnson syndrome
|
|
SE for Felbamate
|
Aplastic anemia and acute hepatic failure
|
|
Anti-seizure medication also used in the prevention of migraines
|
Valproic acid
|
|
Carbamazepine may cause
|
Agranulocytosis
|
|
Anti-seizure drugs used as alternative drugs for mood stabilization
|
Carbamazepine
Gabapentin Lamotrigine & Valproic acid |
|
MOA of general anesthetics
|
Most are thought to act at GABA-A receptor - Chloride channel
|
|
Inhaled anesthetic with a low blood/gas partition coefficient
|
Nitrous oxide
|
|
Inversely related to potency of anesthetics
|
Minimum alveolar anesthetic concentration (MAC)
|
|
Inhaled anesthetics metabolized by liver enzymes which has a major role in the toxicity of these agents
|
Halothane and methoxyflurane
|
|
Most inhaled anesthetics SE
|
Decrease arterial BP
|
|
Inhaled anesthetics are Myocardial depressants
|
Enflurane and halothane
|
|
Inhaled anesthetics cause peripheral vasodilation
|
Isoflurane
|
|
Inhaled anesthetic that may sensitize the myocardium to arrhythmogenic effects of catecholeamines and has produced HEPATITIS
|
HHHHalothane
|
|
Inhaled anesthetic, less likely to lower blood pressure than other agents, and has the smallest effect on respiration
|
Nitrous oxide
|
|
Fluoride released by metabolism of this inhaled anesthetic may cause renal insufficiency
|
Methoxyflurane
|
|
Prolonged exposure to this inhaled anesthetic may lead to megaloblastic anemia
|
Nitrous Oxide
|
|
Pungent Inhaled anesthetic which leads to high incidence of coughing and vasospasm
|
Desflurane
|
|
* DOC for malignant hyper thermia that may be caused by use of halogenated anesthetics
|
* Dantrolene
|
|
i.v. Barbiturate used as a pre-op anesthetic
|
Thiopental
|
|
Benso used adjunctively in anesthesia
|
Midazolam
|
|
* Benzo receptor antagonist, it accelerates recovery from benzo overdose
|
* Flumazenil
|
|
This produces "dissociative anesthesia," is a cardiovascular stimulant which may increase intracranial pressure and hallucinations occur during recover
|
Ketamine
|
|
* Opioid assoc. with respiratory depression but is used in high risk patients who may not survive full general anesthesia
|
* Fentanyl
|
|
State of analgesia and amnesia produced when fentanyl is used w/ droperidol and nitrous oxide
|
Neuroleptanesthesia
|
|
Produces both rapid anesthesia adn recovery, has antiemetic activity and commonly used for outpatient surgery, may cause marked hypotension
|
Propofol
|
|
MOA of Local Anesthetics (LA's)
|
Block voltage-dependent sodium channels
|
|
This may enhance activity of local anesthetics
|
Hyperkalemia
|
|
This may antagonize activity of local anesthetics
|
Hypercalcemia
|
|
Almost all Local anesthetics have this property and sometimes require the administration of vasoconstrictors (ex. Epinephrine) to prolong activity
|
Vasoconstriction
|
|
Local anesthetic with vasoconstrictive property, favored for head, neck and pharyngeal surgery
|
cocaine
|
|
Longer acting local anesthetics which are less dependent on vasoconstrictors
|
Tetracaine & bupivacaine
|
|
These local anesthetics have surface activity
|
Cocaine & benzocaine
|
|
Most important toxic effects of most local anesthetics
|
CNS toxicity
|
|
Commonly abused local anesthetic which has cardiovascular toxicity including severe HTN with cerebral hemorrhage, cardiac arrhythmias, and MI
|
Cocaine
|
|
Local anesthetic causing methemoglobinemia
|
Prilocaine
|
|
Structurally related to acetylcholine, used to produce muscle paralysis in order to facilitate surgery or artificial ventilation. Full doses lead to respiratory paralysis and require ventilation
|
Neuromuscular blocking drugs
|
|
These drugs strongly potentiate and prolong effect of neuromuscular blockade
|
Inhaled anesthetics
Especially isoflurane, aminoglycosides, and antiarrhythmic |
|
These prevent the action of ACh at the skeletal muscle endplate to produce a "surmountable blockade," effect is reversed by cholinesterase inhibitors (ex. neostigmine or pyridostigmine)
|
Nondepolarizing type antagonists
|
|
Agent with long duration of action and is most likely to cause histamint release
|
Tubocurarine
|
|
Non-depolarizing skeletal muscle antagonist that has short duration
|
Mivacurium
|
|
Skeletal muslce agent that can block muscarinic receptors
|
Pancuronium
|
|
Skeletal muscle agent that undergoes Hofmann elimination (breaks down spontaneously)
|
Atracurium
|
|
One depolarizing blocker that causes continuous depolarization and results in muscle relaxation and paralysis, causes muscle pain postoperatively and myoglobinuria may occur
|
Succinylcholine
|
|
During Phase I these agents worsen muscle paralysis by succinylcholine, but during phase II they reverse the blockade produced by succinylcholine
|
Cholinesterase Inhibitors
|
|
Agents acting in the CNS or in the skeletal muscle, used to reduced abnormally elevated tone caused by neurologic or muscle end plate disease
|
Spasmolytic drugs
|
|
Facilitates GABA presynaptic inhibition
|
Diazepam
|
|
GABA agonist in the spinal cord
|
Baclofen
|
|
SImilar to clonidine and may cause hypotension
|
Tizanidine
|
|
* DOC for malignant hyperthermia by acting on the sarcoplasmic reticulum or skeletal muscle
|
* Dantrolene
|
|
Agent used for acute muscle spasm
|
Cyclobenzaprine
|
|
* Irreversible condition resulting from the use o antipsychotics, reserpine at high doses, and MPTP (by-product of illicit meperidine analog)
|
* Drug induced Parkinsonism
|
|
Agent used in drug therapy of Parkinson's instead of Dopamine which has low bioavailability and does not cross the BBB
|
L-dopa
|
|
This is combined with L-dopa, inhibits DOPA decarboxylase (active only peripherally) which allows lower effective doses of L-dopa and allows for fewer SE's (GI distress, postural hypotension, and dyskinesias)
|
Carbidopa
|
|
Clinical response that may fluctuate in tx of Parkinson's dx
|
"On-off Phenomenon"
|
|
Anti-Parkinson's drug which increases intraocular pressure and is C/I in closed angle glaucoma
|
Levodopa
|
|
Ergot alkaloid that is a partial agonist at D2 receptors in the brain, used for patients who are refractory or cannot tolerate levodopa, causes erythromelalgia
|
Bromocriptine
|
|
Non ergot agents used as first-line therapy in the initial management of Parkinson's
|
Pramipexole and ropinirole
|
|
Enhancing dopaminergin neurotransmission SE's include CNS excitation, acute toxic psychosis and Livedo reticularis
|
Amantadine
|
|
Inhibitor of MAO type B which metabolizes dopamine, used adjunct to levodopa or as sole agent in newly diagnosed patients
|
Selegiline
|
|
Inhibitors of chatechol-O-methyltransferase (COMT), used as adjuncts in Parkinson's dx and cause acute hepatic failure (monitor LFT's)
|
Entacapone & Tolcapone
|
|
Agent decreases the excitatory actions of cholnergic neurons. May improve tremor and rigidity but have LITTLE effect on bradykinesia. Atropine-like side effects
|
Benztropine
|
|
Agent effective in physiologic and essential tremor
|
Propranolol
|
|
Agents used Huntington's Disease
|
Tetrabenazine (amine depleting drug)
Haloperidol (anti-psychotic) |
|
Agents used in Tourette's dx
|
Haloperidol or pimozide
|
|
Chelating agent used in Wilson's disease
|
Penicillamine
|
|
Extrapyramidal dysfunction is more common with these agents, which block this subtype of dopamine receptor
|
Older antipsychotic agents, D2 receptors
|
|
MOA of neuroleptics
|
Dopamine blockade
|
|
* Side effects occuring in antipsychotics that block dopamine
|
* Hyper-prolactinemia
Menorrhea Galactorrhea Confusion Mood changes Decreased sexual interest Weight gain |
|
Antipsychotics that reduce positive symptoms only
|
Older antipsychotics
|
|
Newer atypical antipsychotics that also improve some of the negative symptoms and help acute agitation
|
Olanzapine
aripiprazole sertindole |
|
* Antipsychotic used in the treatment of psychiatric symptoms in patients with demetia
|
* Risperidone
|
|
* Atypical antipsychotic causing high prolactin levels
|
* Risperidone
|
|
Newer atypical antipsychotic used for bipolar disorder, known to cause weight gain , and adversely affect diabetes
|
Olanzapine
|
|
Agent more frequently assoc. with extrapyramidal side effects that can be treated w/ benzodiazepine, diphenhydramine, or muscarinic blocker
|
Haloperidol
|
|
* Drug used in neuroleptic malignant syndrome
|
* Dantrolene
|
|
Agents may exacerbate tardive dyskinesias (may be irreversible and there is no treatment)
|
Muscarinic blockers
|
|
* Antipsychotic having the strongest autonomic effects
|
* Thioridazine
|
|
Antipsychotic having the weakest autonomic effects
|
Haloperidol
|
|
Only phenothiazine not exerting antiemetic effects, can cause visual impairment due to retinal deposits, and high doses have been associated with ventricular arrhythmias
|
Thioridazine
|
|
** Agent having no effect on D2 receptors, block D4, reserved for resistant schizophrenia, and can cause fatal agranulocytosis
|
** Clozapine
|
|
* Anti-psychotic not shown to cause tardive dyskinesia
|
* CLozapine
|
|
Anti-psychotics available in depot preparation
|
Fluphenazine and haloperidol
|
|
Reduced seizure theshold
|
Low-potency typical antipsychotics and clozapine
|
|
Orthostatic hypotension and QT prolongation
|
Lowe potency and risperidone
|
|
Increased risk fo developing cataracts
|
Quetiapine
|
|
* Major route of elimination for Lithium
|
* Kidneys
|
|
* Patients being treated with lithium, who are dehydrated, or taking diuretics concurrently, could develop
|
* Lithium toxicity
|
|
Drug inreases th erenal clearance hence decreases levels of lithium
|
Theophylline
|
|
Lithium is associated with this congenital defect
|
Cardiac anomalies adn is contraindicated in pregnancy or lactation
|
|
* DOC for bipolar affective disorder
|
* Lithium
|
|
Concern using lithium
|
Low therapeutic index
|
|
* SE of lithium
|
* Tremor
Sedation Ataxia Aphasia Thyroid enlargement Reversible diabetes insipidus |
|
Examples of 3 antidepressants that are indicated for OCD
|
Clomipramine, fluoxetine adn lfuvoxamine
|
|
NT's affected by the action of antidepressants
|
NE and Serotonin
|
|
Usual time needed for full effect of antidepressant therapy
|
2-3 weeks
|
|
Population group especially sensitive to side effects of antidepressants
|
Elderly patients
|
|
All antidepressants have roughly the same efficacy in treating depression, agents are chosen based on these criterion
|
Side effect profile and prior pt. response
|
|
Well-tolerated and are first -line antidepressants
|
SSRI's
Bupropion Venlafaxine |
|
Most useful in patients with significant anxiety, phobic features, hypochondriasis and resistant depression
|
Monoamine oxidase inhibitors
|
|
Condition will result from in combination of MAOI with tyramine containing foods (ex. wine, cheese adn pickled meats)
|
Hypertensive crisis
|
|
MAOI should not administered with SSRI's or potent TCA's due to development of this condition
|
Serotonin syndrome
|
|
Sedation is a common side effect of these drugs, they lower seizure threshold, uses include BAD, acute panic attacks, phobias, enuresis, and chronic pain and their overdose can be deadly
|
TCA's
|
|
Three C's associated with TCA toxicity
|
Coma
Convulsions Cardiac problems (arrhythmias and wide QRS) |
|
Agents having higher sedation and antimuscarinic effects than other TCA's
|
Tertiary amines
|
|
TCA used in phronic pain, a hypnotic, and has marked antimuscarinic effects
|
Amitriptyline
|
|
* TCA used in chronic pain, enuresis, and ADD
|
* Imipramine
|
|
TCA with greatest sedation of this group adn marked antimuscarinic effects used for sleep
|
Doxepin
|
|
TCA used in OCD most significant of TCA's for risk of seizure, weight gain and neuropsychiatric signs and symptoms
|
Clomipramine
|
|
Secondary amines that have less sedation and more excitation effect
|
Nortriptyline
Desipramine |
|
Side effects seen with tricyclic antidepressants
|
Muscarinic blockade (Dry mouth, constipation)
Weak Alpha1 block (orthostatic hypotension) Weak histamine block (sedation) |
|
Antidepression assoc. with neuroleptic malignant syndrome
|
Amoxapine
|
|
Antidepressant assoc. with seizures and cardiotoxicity
|
Maprotiline
|
|
Antidepressant having stimulant effects similar to SSRI's and can increase BP
|
Venlafaxine
|
|
Antidepressant inhibiting NE, Serotonin, and Dopamine reuptake
|
Venlafaxine
|
|
Antidepressant also used for sleep that causes priapism
|
Trazodone
|
|
Antidepressant which is inhibitor of P450 enzymes and may be assoc. with hepatic failure
|
Nefazoone
|
|
* HCA antidepressant least likely to affect sexual performance, used for management of nicotine withdrawal, SE's include dizziness, dry mouth aggravation of psychosis, and seizures
|
* Buproprion
|
|
Antidepressant with MOA as alpha 2 antagonist, has effects on both 5HT and NE, blocks istamine receptors adn is sedating
|
Mirtazapine
|
|
SE of mirtazapine
|
Liver tox.
Increased serum Cholesterol |
|
Except for these agents all SSRI's have have significant inhibition of P450 enzymes
|
Citalopram and its metabolite escitalopram
|
|
Side effects frequently seen with SSRI's
|
CNS stimulation
GI upset |
|
Antidepressants with no effect on BP, no sedation
|
SSRI's
|
|
SSRI wtih long t1/2 and can be administered once weekly for maintaenance, not acute tx
|
Fluoxetine
|
|
SSRI indicated for premenstrual dysphoric disorder
|
Fluoxetine
|
|
Some SSRI's therapeutic effects beside depression
|
Panic attacks, social phobias, bulimia nervosa, PMDD, & OCD
|
|
SSRI less likely to cause a withdrawal syndrome
|
Fluoxetine
|
|
Inhibit synaptic activity of primary afferents and spinal cord pain transmission neurons
|
Ascending pathways
|
|
* Activation of these receptors close Ca2+ ion channels to inhibit neurotransmitter release
|
* Presynaptic Mu, delta, and kappa receptors
|
|
Activation of these receptors open K+ ion channels to cause membrane hyperpolarization
|
Postsynaptic Mu receptors
|
|
* Tolerance to all effects of opiod agonists can develop except
|
* Miosis and constipation
|
|
All opioids except this agent (which has a muscarinic blocking action) causing pupillary contriction
|
Meperidine
|
|
Se of these drugs incude dependence, withdrawal syndrome, sedation, euphoria, respiratory depression, nausea and vomiting, constipation, biliary spasm, increased ureteral and bladder tone
|
Opioid analgesics
|
|
Strong opioid agonists
|
Morphine
Methadone Meperidine and Fentanyl |
|
Opioids used in anesthesia
|
Morphine and fentanyl
|
|
* Opioid used in the management of withdrawal states
|
* Methadone
|
|
* Opioid available transdermally
|
* Fentanyl
|
|
* Opioid that can be given PO, by epidural adn i.v., which helps to relieve the dyspnea of pulmonary edema
|
* Morphine
|
|
Use of this Opioid with MAOI can lead to hyperpyrexic coma, and with SSRI's can lead to serononin syndrome
|
Meperidine
|
|
* Moderate opioid agonists
|
* Codeine
Hydrocodone Oxycodone |
|
Weak Opioid agonist, poor analgesic, its overdose can cause severe toxicity including respiratory depression, circulatory collapse, pulmonary edema, and seizures
|
Propoxyphene
|
|
Partial Opioid agonist, considering a strong analgesic, has a long duration of action and is reistance to naloxone reversal
|
Buprenorphine
|
|
* Opioid antagonist that is given i.v. and has SHORT DOA
|
* Naloxone
|
|
* Opioid antagonist that is orally in ALCOHOL dependency programs
|
* Naltrexone
|
|
These opioid agents are used as antitussive
|
Dextromethorphan
Codeine |
|
These opioids are used as antidiarrheal
|
Diphenoxylate
Loperamide |
|
Inhalant anesthetics
|
NO, chloroform, and diethyl ether
|
|
Toxic to the Liver, kidney, lungs, BM, peripheral nerves and cause brain damage in anmals, sudden death has occrred following inhalation
|
Fluorocarbons and industrial sovents
|
|
Cause dizziness, Tachycardia, hypotension and flushing
|
Organic nitrites
|
|
Causes acne, premature closure of epiphyses, masculinization in females, hepatic dysfunction, MI, and increases in libido and aggression
|
Steroids
|
|
* Readily detected markers that may assist in diagnosis of the cause of a drug overdose include
|
* changes in heart rate, BP, respiration, body temperature, sweating, bowel signs and pupillary responses
|
|
Most commonly abused in health care professionals
|
Heroin, morphine,oxycodone, perperiine and fentanyl
|
|
Thisroute is associated with rapid tolerane and psychologic dependence
|
i.v. administration
|
|
* Leads to respiratory depression progressing to coma and death
|
* Overdose of opioids
|
|
Lacrimation, rhinorhhea, yawning, sweating, weakness, gooseflesh, N, V, tremor,muscle jerks, and hyperpnrea are signs of this syndrome
|
Abstinence syndrome
|
|
Treatment of opioid addiction
|
Methadone, followed by slow dose reduction
|
|
* This agent may cause more severe, rapid and intense symptoms to a recovering addict
|
* Naloxone
|
|
Sedative-Hypnotics action
|
Reduction inhibition, suppress anxiety, and produce relaxation
|
|
Additive effects when sedative-hypnotics used in combination with these aents
|
CNS depressants
|
|
Common mechanism by which overdose with sedative-hyptnotics resultsin death
|
Depression of medullary and cardiovascular centers
|
|
* "Date rape drug"
|
* Flunitrazepam (rohypnol)
|
|
The most important sign of withdrawal syndrome
|
Excessive CNS stimulation (seizures)
|
|
Tx of withdrawal syndrome involves
|
Long-acting sedative-hypnotic or a gradual reduction of dose, clonidine or propranolol
|
|
*These agents are CNS depressants
|
*Ethanol
Barbiturates Benzo's |
|
Withdrawal from this drug causes lethargy, irritability, ad headache
|
Caffeine
|
|
W/D from this drug causes anxiety and mental discomfort
|
Nicotine
|
|
* Treatments available for nicotine addiction
|
* Patches, gum, nasal spray, psychotherapy, and bupropion
|
|
Chronic high dose abuse of nicotine leads to
|
Psychotic state, OD --> agitation, restlessness, tachcardia, hyperthermia, hyperreflexia, and seizures
|
|
Tolerance is marked and abstinence syndrome occurs
|
Aphetamines
|
|
Amphetamine agents
|
Dextroamphetamines and methamphetamine
|
|
These agents are congeners of Amphetamines
|
DOM, STP, MDA, and MDMA "ecstasy"
|
|
OD's of this agents with powerful vasoconstrictive action may Result in fatalities from arrhythmias, seizures, respiratory depression, or severe HTN (MI and stroke)
|
Cocaine "super-speed"
|
|
Most dangerous of the current popular hallucinogenic drugs, OD leads to nystagmus, marked HTN, and seizures, presenceof both horizontal and vertical nystagmus is pathognomonic
|
PCP
|
|
Removal of PCP may be aided
|
Urinary acidification adn activated charcoal or continual nasogastric suction
|
|
* THC is active ingredient, SE's include impairment of judgement and reflexes decreases in PB and psychomotor performance occur
|
* Marijuana
|
|
* This agent has great affinity for muscarinic receptors and used for postoperative and neurogenic ileus and urinary retention
|
* Bethanechol
|
|
Only direct acting agent that is very lipid soluble adn used in glaucoma
|
Pilocarpine
|
|
This agent used to treat dry mouth in Sjogren's syndrome
|
Cevimeline
|
|
Indirect-aacting ACh Agonist, alcohol, short DOA and used in diagnosis of MG!
|
Edrophonium
|
|
arbamate wtih intermediate action, used for +A170 postoperative and neurogenic ileus and urinary retention
|
Neostigmine
|
|
Treatment of atropine overdose and glaucoma (because lipid soluble). Enters the CNS rapidly and has a timulant effect, which may lead to convulsions
|
Physostigmine
|
|
Tx of MG
|
Pyridostigmine
|
|
Antiglaucoma organophosphate
|
Echothiophate
|
|
Associated with an increased incidence of cataracts in patients treated for glaucoma
|
Long-acting cholinesterase inhibitors
|
|
Scabacide organophosphate
|
Malathion
|
|
Organophosphate antelmintic agent with long DOA
|
Mettrifonate
|
|
* Toxicity of rganophosphate:
|
* DUMBELSS
Diarrhea Urination Miosis Bronchiconstriction Excitation of sk. muscle & CNS Lacrimation Salivation Sweating |
|
The mostfrequent cause of acute deaths in cholinesterase inhibitor toxicit
|
Respiratory failure
|
|
The most toxc organophosphate
|
Parathion
|
|
Tx of choice for organophosphate overdose
|
Atropine
|
|
This agent regenerates active cholineesterase and is a chemical antagonist used to treat organophosphate exposure
|
Pralidoxime
|
|
Prototypical drug is atropine
|
Nonselective Muscarinic Antagonists
|
|
* Treat manifestations of Parkinson's disease and EPS
|
* Benztropine, trihexyphenidyl
|
|
* Treatment of motion sickness
|
* Scopolamined, meclizine
|
|
* Produce mydriasis and cycloplegia
|
* Atpropine, homatropine, C1208 tropicamide
|
|
* Bronchodilateion in asthma and COPS
|
* Ipratroprium
|
|
Reduce transint hyper GI motility
|
Dicyclomine, methscopolamine
|
|
Cystitis, postoperative bladder spasms or incontinence
|
Oxybutynin, dicyclomine
|
|
Tox. of anticholinergics
|
block SLUD (Salivation, lacrimation, urination, defecation)
|
|
Another pneumonic for anticholinergictoxicity
|
Dry as a bone, red as a beet, mad as a hatter, hot as a hare, blind as a ba
|
|
Atropine fever is the most dangerous effect and can be lethal in this population group
|
Infants
|
|
C/I to use of atropine
|
Infants, closed angle glaucoma, prostatic hypertrophy
|
|
Limiting adverse effect of ganglion blockade that patients usueally are unable to tolerate
|
Severe HTN
|
|
Reversal of blockade by Neuromuscular blockers
|
Cholinesterase inhibitor
|
|
Tubocurarine is the prototype, pancuronium, atracurium vecuronium are newer short acting agent, produce cometetive block at end plate nicotinic receptor, causing flaccid paralysis
|
Nondepolarizing Neuromuscular Blockers
|
|
Only member of depolarizing Neuromuscular blocker, causes fasciculation during induction and muscle pain after use; has short duration of action
|
Succinylcholine
|
|
Chemical antagonists that bind to the inhibitor of ACh Estrace and displace the enzyme (if aging has not occurred)
|
Cholinesterase reenerators, Pralidoxime
|
|
Usedto treat pts exposed to insecticides such as parathion
|
Pralidoxime, atropine
|
|
*Pneumonic for beta receptors
|
* you have 1 hart (Beta1) and 2 lungs (beta2)
|
|
* This is the DOC for anaphylactic shock
|
* Epinephrine
|
|
Phenylisopropylamines that are used legitimately and abused for narolepsy, attention deficit disorder adn weight reduction
|
Amphetamines
|
|
Alpha agonist used to produce mydriasis and reduce conjunctival itching adn congestion caused by irritation or allergy, it does not cause cycloplegia
|
Phenylephrine
|
|
Newer alpha2 agonist (apraclonidine adn brimonidine) treat glaucoma by acting to
|
Reduce aqueous secretion
|
|
Short acting beta2 agonists tha tis DOC in tx of acute asthma but not recommended for prophylaxis
|
Albuterol
|
|
Longer acting beta2 agonist is recommended for prophylaxis of asthma
|
Salmeterol
|
|
These agents increase CO and may be beneficial in tx of acute heart failure and some types of shock
|
Beta 1 agonists
|
|
* These agents decrease blood flow or increase BP, are local decongestants adn used in therapy of spinal shock (temporary maintenance of BP which may help maintain perfusion
|
* Alpha1 agonists
|
|
Shock due to septicemia or MI is made worse by
|
Increasing afterload adn tissue perfusion declines
|
|
Epinephrine is often mixed with a local anesthetic to
|
reduce the loss from area of injection
|
|
Chronic orthostati hypotension can be treated with
|
Midrodrine
|
|
Beta2 agonist used to suppress premature laboe, but cardiac stimulatory effects may be hazardous to mother and fetus
|
Terbutaline
|
|
Sympathetic agent which stimulates HR and can dilate vessels in skeletal musce at slow doses
|
Epinephrine
|
|
Mast cells to recuce release of Histamine and inflammatory mediators
|
Epinephrine
|
|
Agent used in shock b/c it dilates coronary arteries and increases renal blood flow
|
Dopamine
|
|
Agent which stimulates cardiac contractileforce more than rate with little effect on total peripheral resistance
|
Dobutamine
|
|
Long cting sympathomimetic, sometimes used to improve urinary coninence in kids and elderly with enuresis
|
Ephedrine
|
|
* Alpha 1 agonist toxicity
|
* Hypertension
|
|
Beta 1 agonist toxicity
|
Sinus tachy, and serious arrhythmias
|
|
Beta 2 agonist toxicity
|
Skeletal muscle tremor, tachycardia
|
|
The selective agents loose their selectivity at
|
high doses
|
|
Nonselective alpha-blocker drug, long acting and irreversible and used to treat pheochromocytoma.
Blocks 5HT so occasionally used for carcinoid tumor. Blocks H1 and used in mastocytosis |
Phenoxybenzamine
|
|
Nonselective alpha-blocking drug, short acting and reversible used for rebound HTN from rapid clonidine withdrawal adn Raynaud's phenomena
|
Phentolamine
|
|
* Selective alpha 1 blocker used for HTN, BPH may cause first dose orthostatic hypotension
|
* Prazosin
Terazosin Doxazosin |
|
Selective alpha 1A blockerm used for BPH but with little effect on HTN
|
Tamulosin
|
|
Selective alpha 2 blocker used fo rimpotence
(controversial effectiveness) |
Yohimbine
|
|
* SelectiveB1 receptor blockers that may be useful in treating patients even though they have asthma
|
* Acebutolol
Atenolol Esmolol Metoprolol |
|
Combined alpha and beta blocking agents that may have application in treatment of CHF
|
Labetalol and carvedilol
|
|
Beta blockers partial agonist activity (intrinsic sympathomimmetic activity) cause some bronchidilation adn may have an advantage in treating pts with asthma
|
Pindolol and acebutolol
|
|
* This beta blocker lacks local anesthetic activity (a property which decreases protective reflexes and increases the risk of corneal ulceration) and used in treating glaucoma
|
* Timolol
|
|
This parenteral beta blocker is a short acting (minutes)
|
Esmolol
|
|
THis beta blocker is th longest acting
|
Nadolol
|
|
These beta blockers are less lipid soluble
|
Acebutolol and atenolol
|
|
This beta blocker is highly lipid soluble and may account for side efects such as NIGHTMARES!
|
Propranolol
|
|
Clinical uses of these agents include tx of HTN, angina, arrhythmias, chronic CHF and selected post MI patents
|
Beta blockers
|
|
Tox. of these agents include bradycardia, AV block, exacerbation of acute CHF; signs of hypoglycemia may be masked (tachy, tremor, and anxiety)
|
Beta blockers
|
|
Cholinomimetics that increase outflow, open trabecular meshwork, and cause ciliary muscle contraction
|
Pilocarpine
carbachol physostigmine |
|
Nonselective alpha agonists that increases outflow, probably cia the uveoscleral veins
|
Epinephrine, dipivefrin
|
|
Selective alpha agonists that decreases aqueous secretion
|
Apraclonidine
brimonidine |
|
* These beta blockers decrease aqueous secretion
|
* Timolol (nonselective)
Betaxolol (selective) |
|
This diuretic decreases aqueous secretion due to lack of HCO3- ion. Causes drowsiness and paresthesias, alkalinization of the urin may precipitate Ca salts, hypokalemia, acidosis
|
Acetazolamide
|
|
This agent causes increased aqueous outflow
|
Prostaglandin PGF2a
|
|
* Inhibits ACE
|
* ACE inhibitors
|
|
* Captopril and enalapril (-OPRIL ending) are
|
* ACE inhibitors
|
|
* SE of ACE inhibitors
|
* Dry cough, hyperkalemia
|
|
* ACE inhibitors are contraindicated in
|
* pregnancy adn with K+
|
|
* Losartan adn valsartan block
|
* Angiotensin receptor
|
|
* Angiotensin receptor blockers do NOT cause
|
* Dry cough
|
|
Agents that block L-type calcium channel
|
Ca channel blockers
|
|
* CCB contraindicated in CHF
|
* Verapamil
|
|
CCB with predominate effect on arteriole dilation
|
Nifedipine
|
|
* SE of CCB
|
* Constipaton, edema and headache
|
|
* Agents that reduce HR, contractility and O2 demand
|
* Beta-blockers
|
|
B-blockers that are more cardioslective
|
Beta-1 slective blockers
|
|
* Cardioselective beta1 blockers
|
* Atenolol
Acebutolol Metoprolol |
|
Beta-blockers should be used cautiously in
|
Asthma (bronchospasmic effects)
Diabetes (block igns of hypoglycema) Peripheral Vascular disease |
|
Non-selective betablocker also used for migraine prophylaxis
|
Propranolol
|
|
* SE of betablockers
|
* Bradycardia
SEXUAL DYSFUNCTION Decreased HDL Increased TG's |
|
* Alpha 1 selective blockers
|
* - AZOSIN endings
Prazosin Terazosin Doxazosin |
|
Non-selective alpha1 blockers used to treat pheochromocytoma
|
Phenoxybenzamine
|
|
For rebound HTN form rapid clonidine withdrawal
|
Phentolamine
|
|
* A1a-selective blocker with no effects on HTN used for BPH
|
* Tamsulosin (Flomax)
|
|
* SE of alpha blockers
|
* Orthostatic hypotension (esp with first dose
+ Reflex tachycardia |
|
Presynaptic Alpha 2 agonist used in HTN adn acts centrally
|
Clonidine and methyldopa
|
|
SE of methyldopa
|
Positive coomb's test, depression
|
|
* Methyldopa is C/I in
|
* Geriatrics due to itsCNA (depression) effects
|
|
SE of clonidine
|
Rebound HTN, sedation, dry mouth
|
|
Direct vasdilator of arteriolar smooth muscle
|
Hydralazine
|
|
* SE of hydralazine
|
* Lupus-like sundrome
|
|
Arterial vasodilator tha tworks by opening K+ channels
|
Minoxidil
|
|
SE of minoxidil
|
Hypertrichosis
|
|
IV drug used hypertensice crisis
|
Nitroprusside
|
|
Nitroprusside vasodilates
|
Arteries and veins
|
|
Toxicity caused by nitroprusside and treatment
|
Cyanide toxicity treated with sodium thiosulfate
|
|
Caronic anhydrase inhibitor
|
Acetazolamide
|
|
* Diuretic used for mountain sickness and glaucoma
|
* Acetazolamide
|
|
* SE of acetazolamide
|
* Paresthesias, alkalinization of the urine (which may precipitate Ca salts), hypokalemia, acidosis, and encephalopathy in pts wiht hepatic impairment
|
|
MOA of loop diuretics
|
Inhibits Na/K/2Cl CO transporter
|
|
* Site of action of loop diuretics
|
* Thick ascending limb
|
|
* SE of loop (furosemide) diuretics
|
* Hyperuricemia
Hypokalemia Ototoxicity |
|
Aminoglycosides used with loop diuretics potentiate adverse effect
|
Ototoxicity
|
|
* Loops lose and thiazide's retain..
|
* Calcium
|
|
MOA of Thiazides
|
Inhibit Na/Cl CO transport
|
|
* Site of action of thiazide diuretics
|
* Work at early DCT
|
|
Class of drugs that may case cross-sensitivity with thiazide diuretics
|
Sulfonamides
|
|
* SE of thiazides (HCTZ) diuretics
|
* Hyperuricemia
Hypokalemia Hyperglycemia |
|
* K sparing diuretics inhibit
|
* Na/K exchange
|
|
* Diuretic used to treat primary aldosteronism
|
* Spironolactone
|
|
* SE of Spironolactone
|
* Gynecomastia, hyperkalemia, and impotence
|
|
* Osmotic diuretic used to treat increased intracranial pressure
|
* Mannitol
|
|
* ADH agonist used for pituitary diabetes insipidus
|
* Desmopressin (DDVAP)
|
|
Used for SIADH
|
Demeclocycline
|
|
SE of demeclocycline
|
Bone marrow and teethc discoloration for children under 8 years ofage
|
|
* MOA of class IA (eg. Procainamide), class IB (eg. Lidocaine), and class IC (eg. Flecainide) antiarrhythmics
|
* Sodium Channel blockers
|
|
* SE of procainamide
|
* Lupus-like syndrome
|
|
* Limiting SE of Quinidine
|
* Prolongs QT interval
|
|
Other side effects of Quiniine
|
Thrombocytopoenic purpura and CINCHONISM
|
|
Major drug interaction w/ Quinidine
|
Increases conc. of Digoxin
|
|
* DOC for management of Acute Ventricular Arrhythmias
|
* Amiodarone
|
|
DOC for digoxin inducedarrhythias
|
Phenytoin
|
|
SE of phenytoin
|
Gingical hyperplasia
|
|
Class of anti-arrhythmics that has a pro-arrhythmic effect (CAST trial), therefore are used as last line agents
|
Class IC (Flecainide, propafenoone, moricizine)
|
|
Class II antiarrhythmics are
|
B-Blockers
|
|
Antiarrhythmic that exhibits Class II and III properties
|
Sotalol
|
|
SE of sotalol
|
prolongs QT and PR interval
|
|
Used i.v. for acute arrhythmias during surgery
|
Esmolol
|
|
Anti-arrhythmics that decrease mortality
|
B-blockers
|
|
MOA of Class III antarrhythmics
|
Potassium channel blockers
|
|
Class III antiarrhythmic that exhibits properties of all 4 classes
|
Amiodarone
|
|
Specific pharmacokinetic characteristic of amiodarone
|
Prolonged half-life, up to 6 weeks
|
|
Antiarrhythmic effective in most type os arrhythmias
|
Amiodarone
|
|
SE of Amiodarone
|
Cardiac dysfxn
Photosensitivity Skin (blue smurf syndrome) Pulmonary fibrosis Thyroid and corneal deposits |
|
MOA of class IV antiarrhythmics
|
Calcium channel blockers
|
|
* LIfe threatening cardiac event that prolong QT leads to
|
* Torsades de pointes
|
|
Agent to treat torsades de pointes
|
Magnesium Sulfate
|
|
Drug used for supraventricular arrhythmias
|
Digoxin
|
|
DOC for paroxysmal supraventricular tachycardia
|
Adenosine
|
|
Adenosine's MOA
|
Activation of an inward K+ current and inhibition of Ca2+ current resulting in marked hyperpolarization
|
|
Anti-arrhythmic wtih 15 second DOA
|
Adenosine
|
|
*** MOA of sildenafil (Viagra)
|
*** Inhibits phosphodiesterase-5, enhancing effects of Nitric oxide-activated increases in cGMP
|
|
Drugs used in the management of angina
|
Aspirin
Nitrates CCB B-blockers |
|
Aspirin reduces mortality in unstable andinga by...
|
Platelet aggregation inhibition
|
|
* MOA of nitrates
|
* Relaxes vascular smooth muscle, at low doses dilate veins and at high doses dilates arterioles
|
|
Nitrate used for Acute anginal attacks
|
Nitroglycerin sublinual tablets
|
|
Nitrate used to prevent further attacks
|
Oral and transdermal forms of nitroglycerin
|
|
Nitrate free intervals are needed due to
|
Tolerance
|
|
SE of nitrates
|
- Postural hypotension
- Reflex tachy - hot flashes - throbbing headache due to meningeal artery dilation |
|
CCB are DOC for
|
Prinzmetal's angina
|
|
Beta blockers are used for which type of anginal attack
|
Classic
|
|
MOA of Cardiac glycosides (eg. digoxin)
|
Indirectly increases intracellular Ca and cardiac contractility by inhibiting Na/K/AATPase
|
|
Digoxin is used in...
|
Atrial Fibrillation and CHF
|
|
Digoxin toxicity can be precipitated by
|
hypokalemia
|
|
Antidote for digoxin toxicity
|
Dgibind
|
|
Phosphodiesterase inhibitors that increase mortality and have been found to have NO beneficial effects
|
Amrinone and Milrinone
|
|
SE of amrinone
|
Thrombocytopenia
|
|
Beta1 agonists used in Acute CHF
|
Dobutamine & Dopamine
|
|
Diuretics work in CHF by
|
Reducing PRELOADDDDD
|
|
B-blockers work in CHF by
|
Reducing progression of heart failure
(Never use in acute heart failure) |
|
Peptide drug used to treat CHF
|
Nesiritide (BNP)
|
|
MOA of nesiritide
|
Increasing Na excretion adn decreases arterial and venoud tone
|
|
SE of nesiritide
|
Excessive hypotension and kidney failure
|
|
Agent used in CHF that is a selective alpha and nonselective beta blocker
|
Carvedilol
|
|
Agent used in acutely decompensated CHF resembling natriuretic peptide
|
Nesiritide (Natrecor)
|
|
* Vitamin K dependent anticoagulation
|
* Warfarin (PT)
|
|
Warfarin in contraindicated in..
|
PREGNANCY
|
|
Anticoag of choice in pregnancy
|
HEPARIN (PTT)
|
|
* Heparin (PTT) increaes activity of
|
* ntithrombn 3
|
|
Route of administration of warfarin
|
ORAL
|
|
Routes of administration of Heparin
|
i.n. and i.m. (only LMW)
|
|
SE of both warfarin adn heparin
|
Bleeding
|
|
SE of Heparin
|
Heparin induced thrombocytopenia (HIT)
|
|
Alternative to nticoagulant used if HIT develops
|
Lepirudin
|
|
Antidote to reverse actions of Warfarin
|
Vitamin K ro FFP
|
|
* Antidote to reverse the actions of Heparin
|
* Protamine Sulfate
|
|
MOA of aspirin
|
Irreversibly blocks cyclooxygenase
|
|
Agent used to treat MI and to reduce icidence of subsequent MI
|
Aspirin, metoprolol
|
|
* SE of Aspirin
|
* GI bleeding
|
|
Antiplatelet drug reserved for patients allergic to aspirin
|
Ticlodipine
|
|
SE of ticlodipine
|
Neutropenia and agranulocytosis
|
|
Effective in preventing TIA's
|
Clopidogrel & Ticlopidine
|
|
Prevents thrombosis in pts with artificial heart valve
|
Diyridamole
|
|
Block glycoprotein IIb/IIIa invlved in platelet cross-linking
|
Abciximab, Tirofiban, & eptifibatide
|
|
* MOA of thrombolytics
|
* Degradation of fibrin clots and are administered i.v.
|
|
* Thrombolytics are used for
|
* Pulmonaty embolism and DVT
|
|
Thrombolytic that can cause allergic rxn
|
Streptokinase
|
|
THrombolytic use for acute MI and ischemic (non-hemorrhagic) CVA
|
t-PA
|
|
Se of t-PA
|
Cerebral hemorrhage
|
|
Antidote for thrombolytics
|
Aminocproid acid
|
|
Agent to treat hypochromc microcutic anemias
|
Ferrous Sulate
|
|
Chelating agent used in acute iron toxicity
|
Deferoxaine
|
|
* Agent for pernicious anemia
|
* Cyanocobalamin (Vit. B12)
|
|
Agent used for neurological deficits in Megaloblasitc anemia
|
Vitamin B12
|
|
* Agent used for megaloblastic anemia (but does NOT reverse neurological sx) and decrease NTD's during pregnancy
|
* Folic acid
|
|
* Agent used for anemias assoc. with renal failure
|
* Erythropoietin
|
|
Agent used neutropenia esp after chemoterapy
|
G-CSF (FIlgrastim) adn GM-CSF (sargramostim)
|
|
Tx of pts wiht prior episodes of thrombocytopenia after a cycle of cancer chemo
|
IL-11
(oprelvekin) |
|
Drugs decrease intestinal absorption of cholsterol
|
Bile acid-binding resins
|
|
Cholestyramine & colestipol are
|
Bile acid-binding resins
|
|
Major nutritional SE of bile acid-binding resins
|
Impair absorption of fat soluble vitamin absorption (ADEK)
|
|
MOA of Lovastatin (STATIN)
|
Inhibits HMG COA reductase
|
|
HMG CoA reductase inhibitors are C/I/ in
|
Pregnancy
|
|
* MOA of drug or foods (grapefruit juice) that increase statin effect
|
* Inhibit cyp450 3A4
|
|
SE of HMG COA reductase inhibitors
|
Rhabdomyolysis and hepatotoxicity
|
|
* Monitoring parameter to obtain before initiation of STATINS
|
* LFT's
|
|
* Decreases liver TG synthesis
|
* Niacin
|
|
* SE of niacin
|
* Cutaneous flush
|
|
Cutaneous flush can be reduced by pretreatment with
|
Aspirin
|
|
* Fibrates (gemfibrozil) increase activity of
|
* Lipoprotein lipase
|
|
Most common SE of fibrates
|
Nausea
|
|
Fibrates are C/I in
|
Pregnancy
|
|
Concurrent use of fibrates and statins increases risk of
|
Rhabdomyolysis
|
|
New class of drugs that works by inhibiting absorption of intestinal cholesterol and can be given concurrently with Statins
|
Ezetimibe
(Zetia) |
|
MOA of NSAIDs
|
Inhibiting prostaglandin sythesis by inhibiting cyclooxygenase (COX)
|
|
Difference between aspirin adn other NSAIDs
|
Aspirin irreversibly inhibits COX, the others reversibly inhibit
|
|
Four main actions of NSAIDs
|
Anti-inflammatory
Analgesia ntipyretic Antiplatelet activity |
|
* Agent used for closure of Patent ductus arteriosus
|
* Indomethacin
|
|
Aspirin is C/I in children with viral infection
|
Potential for developing Reye's syndrome
|
|
SE of salicylates
|
Tinnitus
GI bleeding |
|
NSAID also available as an ophthalmic preparation
|
Diclofenac
Ketorolac |
|
NSAID available ORALLY, IM and ophthalmically
|
Ketorolac
|
|
Concurrent use of fibrates and statins increases risk of
|
Rhabdomyolysis
|
|
New class of drugs that works by inhibiting absorption of intestinal cholesterol and can be given concurrently with Statins
|
Ezetimibe
(Zetia) |
|
MOA of NSAIDs
|
Inhibiting prostaglandin sythesis by inhibiting cyclooxygenase (COX)
|
|
Difference between aspirin adn other NSAIDs
|
Aspirin irreversibly inhibits COX, the others reversibly inhibit
|
|
Four main actions of NSAIDs
|
Anti-inflammatory
Analgesia ntipyretic Antiplatelet activity |
|
* Agent used for closure of Patent ductus arteriosus
|
* Indomethacin
|
|
Concurrent use of fibrates and statins increases risk of
|
Rhabdomyolysis
|
|
Aspirin is C/I in children with viral infection
|
Potential for developing Reye's syndrome
|
|
New class of drugs that works by inhibiting absorption of intestinal cholesterol and can be given concurrently with Statins
|
Ezetimibe
(Zetia) |
|
MOA of NSAIDs
|
Inhibiting prostaglandin sythesis by inhibiting cyclooxygenase (COX)
|
|
SE of salicylates
|
Tinnitus
GI bleeding |
|
Difference between aspirin adn other NSAIDs
|
Aspirin irreversibly inhibits COX, the others reversibly inhibit
|
|
Concurrent use of fibrates and statins increases risk of
|
Rhabdomyolysis
|
|
NSAID also available as an ophthalmic preparation
|
Diclofenac
Ketorolac |
|
Four main actions of NSAIDs
|
Anti-inflammatory
Analgesia ntipyretic Antiplatelet activity |
|
New class of drugs that works by inhibiting absorption of intestinal cholesterol and can be given concurrently with Statins
|
Ezetimibe
(Zetia) |
|
NSAID available ORALLY, IM and ophthalmically
|
Ketorolac
|
|
MOA of NSAIDs
|
Inhibiting prostaglandin sythesis by inhibiting cyclooxygenase (COX)
|
|
* Agent used for closure of Patent ductus arteriosus
|
* Indomethacin
|
|
Aspirin is C/I in children with viral infection
|
Potential for developing Reye's syndrome
|
|
Difference between aspirin adn other NSAIDs
|
Aspirin irreversibly inhibits COX, the others reversibly inhibit
|
|
SE of salicylates
|
Tinnitus
GI bleeding |
|
Four main actions of NSAIDs
|
Anti-inflammatory
Analgesia ntipyretic Antiplatelet activity |
|
NSAID also available as an ophthalmic preparation
|
Diclofenac
Ketorolac |
|
* Agent used for closure of Patent ductus arteriosus
|
* Indomethacin
|
|
NSAID available ORALLY, IM and ophthalmically
|
Ketorolac
|
|
Aspirin is C/I in children with viral infection
|
Potential for developing Reye's syndrome
|
|
SE of salicylates
|
Tinnitus
GI bleeding |
|
NSAID also available as an ophthalmic preparation
|
Diclofenac
Ketorolac |
|
NSAID available ORALLY, IM and ophthalmically
|
Ketorolac
|
|
Concurrent use of fibrates and statins increases risk of
|
Rhabdomyolysis
|
|
New class of drugs that works by inhibiting absorption of intestinal cholesterol and can be given concurrently with Statins
|
Ezetimibe
(Zetia) |
|
MOA of NSAIDs
|
Inhibiting prostaglandin sythesis by inhibiting cyclooxygenase (COX)
|
|
Difference between aspirin adn other NSAIDs
|
Aspirin irreversibly inhibits COX, the others reversibly inhibit
|
|
Four main actions of NSAIDs
|
Anti-inflammatory
Analgesia Antipyretic Antiplatelet activity |
|
* Agent used for closure of Patent ductus arteriosus
|
* Indomethacin
|
|
Aspirin is C/I in children with viral infection
|
Potential for developing Reye's syndrome
|
|
SE of salicylates
|
Tinnitus
GI bleeding |
|
NSAID also available as an ophthalmic preparation
|
Diclofenac
Ketorolac |
|
NSAID available ORALLY, IM and ophthalmically
|
Ketorolac
|
|
NSAID that is used for acute condition, such as preop anesthesia a has limited duration (<5 days) of use due to nephrotoxicity
|
Ketorolac
|
|
Newer NSAID that selectively inhibits COX-2
|
Celecoxib
|
|
COX 2 inhibitors may have reduced risk of
|
Gastric ulcers and GI bleeding
|
|
COX 2 inhibitors should be used cautiously in pts with
|
Pre-existing cardiac or renal disease
|
|
* Acetaminophen only has
|
* Antipyretic and analgesic activity
|
|
SE of acetaminophen
|
Hepatotoxicity
|
|
* Antidote for acetaminophen toxicity
|
* N-acetylcysteine
|
|
* DMARDs are slow acting drugs for
|
* Rheumatic disease
|
|
Initial DMARD of choice for patients with RA
|
Methotrexate
|
|
Drug often used in combo w/ TNF-alpha inhibitors for RA
|
Methotrexate
|
|
Causes BM suppression
|
Methotrexate
|
|
SE of penicillamine
|
Aplastic anemia & Renal toxicity
|
|
Interferes with activity of T-lymphocytes
|
Hydroxychloroquine
|
|
Anti-malarial drg used in RA
|
Hydroxychloroquinine
|
|
SE of Hydroxychloroquinine
|
Retinal destruction and dermatitis
|
|
MOA of Leflnomide (newer agent)
|
Inhibiting dihydroorate dehydrogenase which leads to decreased pyrimidine synthesis, decreased T call proliferation adn decreased antibody production by B cells
|
|
Proteins that prevent action of TNF-alpha
|
Adalimumab
Ifliximab Etanercept |
|
Anti-rheumatic agent also used for ulerative colitis
|
Sulfasalazine
|
|
Anti-rheumatic agent also used for Chrohn's disease
|
Infliximab
|
|
* NSAID used in Gout
|
* Indomethacin
|
|
NSAID C/I in gout
|
Aspirin!
|
|
MOA of colchicine (used in acute gout)
|
Selective inhibitor of microtubule assenbly
|
|
SE of colchicine
|
Kidney and liver toxicity, diarrhea
|
|
Agents used to treat chronic gout by increasing uric acid secretion and excretion
|
Probenecid and sulfinpyrazone
|
|
* Allopurinol treas chronic gout by decreasing uric acid production by inhibiting...
|
* Xanthine oxidsae
|
|
** Rapid acting insulins that do not self-aggregate
|
** Lispro insulin
Aspart insulin Glulisine insulin |
|
** Peakless ling action insulin
|
** Insulin glargine
|
|
DOC for paroxysmal supraventricular tachycardia; has high efficacy and short duration of action
|
Adenosine
|
