Pharmacology Test 2

Heart Failure Drugs

Improve cardiac blood flow

Reduce blood volume (1st prescribed for high blood pressure)

Control heart rhythm

Reduce blood clotting

Reduce lipids

Contraction of the heart

resting of the heart

SA Node

Blood Pressure

Systolic pressure (CO mainly determines systolic BP)

Diastolic pressure (PVR mainly determines diastolic BP)

Preload (determined by the force of venous return)

Diuretics effect preload

Contractility

Afterload

AV Node

SA Node

Junctional Area

affect the force of contraction

-used for heart failure
-increase the force of contraction

-slow the force of contraction

affect the heart rate

increase the rate

decrease the rate

affect the conduction of the electrical impulses through the heart

enhance the conduction of electrical impulses in the heart

decrease the conduction of electrical impulses in the heart

ejection fraction

Calcium!

Heart Failure

-Increase the force of the contraction and thus increase CO
-Positive inotropic drugs and negative chronotropic and negative dromotropic
-must take apical pulse for 1 minute and can not give if under 50 bpm
-oldest and most effective group of drugs
-originally derived from the digitalis lanta plant

-Positive Inotropics that inhibit the enzyme phosphodiesterase whih increases force of contraction by increasing the amount of Ca+ available.
-ONLY USED IN HEART FAILURE
-Vasodilator
Not used much an more
-must be on monitor because causes dysrhythmias

-Used for CHF and dysrhythmias
-Adverse effects due to narrow therapeutic window (Bradycardia, vision changes, n/v)
-Therapeutic level is 0.5 to 2 mg/dl
-Long half-life (up to 3 days)
NUMEROUS DRUG INTERACTIONS

The renin system casues the release of aldosterone to cause vasoconstriction and Sodium retention and Potassium excretion to cause increased blood volume BUT intervening causes no release of aldosterone and no vasoconstriction to keep BP low!!!

-blocks enzyme involved in conversion of angiotension 1 to angiotensin 2
-inhibits aldosterone secretion (vasoconstrictor) and inhibits breakdown of bradykinin (vasodilator)
-these drugs end in -RIL
-40% develop DRY COUGH that is releated to the inhibition of bradykinin breakdown

-Angiotensin 2 Receptor Blockers
-similar to ACE but dont cause cough
-end in -SARTAN

-blocks aldosterone receptors in the heart and blood vessels
-used in heart failure

-blocks renin release from the kidneys
-very new and possibyl not used much due to price

-drugs used in the management of angina
-Dilate vessels and thereby increase supply of oxygen to the heart
-decrease the workload of the heart to decrease the demand for oxygen
-CHF related angina treated with the same drugs

Angina

Chronic stable angina

Unstable angina (preinfartion angina)

Vasospastic angina

-minimize frequency of attacks and decrease duration and intensity
-improve patients functional capacity with few side effects
-prevent or delay worst possible outcome

-nitrates/nitrites
-beta blockers
-calcium channel blockers

-dilate all blood vessels, especially coronary arteries
-adverse effect: reflex tachycardia, severe hypotension
-prototype: Nitroglycerin which is rapid acting and has large first-pass effect so given SL

-decrease myocardial oxygen demand by decreasing heart rate and contractility
-protects heart from SNS and dysrhythmias
-decreases contractility
-Adverse effects: bronchial constriction if not cardioselective
-prototype: metaprolol (cardioselective)

Vasodilation and increased blood flow=decrease demand for oxygen
-types: heart and vessel specific
Adverse Effects: decreased bp, and bradycardia
-new designer calcium channel blocker targeted specifically for vasculature in the brain (lipophilic to cross BBB and good for migraines)

-newest drug developed by DNA technology
-short term, IV for severe heart failure ONLY

-three peptides that provide protection to the CV system in overload.
-Action: released when blood volume is excessive
-lowers pressure by reducing blood volume and shifts fluid to the intravascular compartment (edema)
-lab tests for: elevated suggest too much fluid or says how treatment is going.

Antidysrhythmic drugs
-not used much anymore because they can worsen an exsisting dysrhythmia and generate new ones.

Dysrhythmias

-Class I or sodium channel blockers
-Class II or beta blockers
-Class III or potassium channel blockers
-Class IV or calcium channel blockers

-inhibit movement of sodium
-Divided into Ia, Ib, and Ic

-fast sodium channel blockers
-slows conduction and prolongs repolarization
-use: atrial fib is example
-Prototype: quinidine

-used for premature ventricular contractions ONLY
-Action: slows conduction and shortens repolarization
-Prototype: Lidocaine

-most potent
-slow the conduction rate through the atria and ventricles with no effect on repolarization
-use: severe ventricular dysrhythmias
-prototypes: Encainide

-beta blockers
-action: prevent stimulation of beta cells of the SNS of the heart; reduces calcium entry
-use: ventricular dysrhythmias

-potassium channel blockers
-Action: slows the rate of electrical conduction and prolongs repolarization
-use: life threatening
ventricular tachycardia or fibrillation
-limited use due to side effects (damage lungs)

-calcium channel blockers
-action: blocks Ca+ channels, slows conduction through the AV node to slow heart rate
-use: supraventricular tachycardia
-SE: hypotension, dizzimess

-Drug that promotes the excretion of urine
-increase the removal of sodium and water from the body
-used for the treatment of hypertension and heart failure (decrease Extracellular volume), intraocular pressure
-most are safe but can cause electrolyte/fluid imbalance
-many times combined with antihypertensive drugs in one pill

1. Carbonic anhhydrase inhibitors
2. Loop Diuretics
3. Osmotic diuretics
4. Potassium Sparing diuretics
5. Thiazide and Thiazide-like diuretics

-sulfonamide antibiotic derivatives-weak and not used often because better ones have been developed
-Action: inhibits enzyme carbonic anhydrase in the proximal tube (enzyme responsible for reabsorption of sodium and bicarbonate)
-main use is in the treatment of glaucoma
-Adverse effect: Acidosis

-work in the Loop of Henle
-must watch potassium levels
-Action: inhibit reabsorption of sodium and cholride in teh ascending loop of henle
-use: edema associated with CHF
-Adverse effects: dizziness, n/v, HYPOKALEMIA
-Prototype: furosemide (Lasix)

Action: Proximal tubule action. Pull water into blood vessels and nephrons and ultimately increases urine production.
-NOT FOR CHF patients!!
-Use: intracranial edema, intraocular pressure (used for head injuries)

-Aldosterone antagonists: block aldosterone action in distal nephron so K+ is retained and sodium excreted. Used for CHF in children and reversal of K+ loss produced by other diuretics
Adverse effects: HYPERKALEMIA
-Non aldosterone antagonists: disrupts sodium potassium exchange by directly blocking exchange.
-use: hypertension and edema

-derivatives of sulfonamides
-action: Inhibit Na+, water, Cl-and K+ reabsorption in the ascending loop of henle and early distal tubule
-have a ceiling effect
-used widely for hypertension
-Adverse effects: hypokalemia

Louis Pasteur

Paul Erlich

Sir Alexander Fleming

Antibacterial

Antimicrobial

Antibiotic

Anti-infective

Bacteriostatic

Bacteriocidal

-by organism
-by use
-by chemical structure
-by mechanism of action

-Antibacterial (narrow spectrum, broad spectrum, mycobacteria, extended spectrum)
-Antivial (drugs for HIV, drugs for influenza, other)
-Antifungal
-Antiparasitic
-Antihelmintic (for worms)

-treat illness
-prevent illness

-cell wall inhibitors
-protein synthesis inhibitors
-inhibitors of synthesis of DNA or RNA
-Antimetabolites

Overuse of antibiotics causing resistance

-produce an enzyme to deactivate the drug
-change cellular permeability to prevent entry or alternating of transport system
-alter binging sites on membranes so they no longer accept drug
-produce drug antagonist chemical

-methicillin resistant staphylococcus aureus (MRSA)
-Methicillin resistant staphylococcus epidermis (MRSE)
-Penicillin resistant streptococcus pneumoniae
-Vancomycin resistant enterococci (VRE)
-Multiple drug resistant Tuberculosis (MDR-TB)

-limit use to agents specific for pathogen
-highest does for longest period of time
-COMPLETE THE DRUG!!
-education!
-DO NOT use a more powerful drug when a less powerful drug is just as effective

-Culture and Sensitivity done before starting antibiotic
-keeping levels up (keep doses on time, peak and trough levels)

drawn minutes after IV antibiotic completed to prevent toxicity

drawn immediately prior to the next IV given to measure elimination

-Age groups (infant/children-early exposure leads to sensitivity; pregnancy-most category B and C; elderly)
-Drug interactions
-Toxicity
-Allergies (hypersensitivity and cross sensitivity)
-Superinfections

-All are bacteriocidal
-Beta-Lactam Antibiotics (beta lactam ring)
-Vancomycin
-Isoniazid
-Betalactamase (penicilinase) inhibitors (betalactamase is an enzyme produced by some bacteria that break down the beta lactam ring and is always paired with penicillin)

-Penicillin
-Cephalosporins
-Carbapenems
-Monobactams

-weaken bacterial cell wall, water enters, organism dies
-generally bacteriocidal
-some are penicillinase resistant
-one of the safest
-braod, narrow, or extended spectrum
-Use: prevention and treatment of wide range of bacterial infections (DONT CROSS BBB)
-Nursing care: take with water 2 hours before or after eating and monitor for 30 minutes after

-largest class with over 20 drugs
-four generations: first generation beta-lactamase bacteria will be resistant and 3rd and 4th generation cross BBB to treat CNS infections
-very safe
-broad spectrum
-same uses as penicilin (dont give if allergic to penicilin)
-Nursing Care: oral forms should be given with food to decrease GI upset but will delay absorption

-"last resort" for very serious infections
-can cause seizures
-no cross sensitivity with penicillin

-no cross sensitivity with penicillin
-narrow spectrum to gram negative
-bacteriocidal
-use: systemic infection, UTI
-ADVERSE EFFECTS: NEPHROTOXIC
-IM or IV only
-Nursing care: look at kidney function labs before being on drug

-narrow spectrum
-binds to cell wall and alters permeability results in death
-use: DOC in MRSA, gm + microbes, c diff, staph, strep.
-some bacteria resistant (VRE)
-IV administration too rapid=red man syndrome

-generally bacteriostatic
-Action: inhibit protein synthesis by binding to ribosomal unit in the cell and bacterial stops growth
-Tetracyclines
-Macrolides
-Aminglycosides
-Lincosamides
-Cloramphenicol
-Oxazolidinones

-used when allergy to penicillin
-made from strep
-broad spectrum
-use: pneumonia, acne, H pylori
-CANT USE IN CHILDREN
-Adverse effects: teeth dicoloration in unborn an dkids, photosensitivity (sunburn)
-Interactions: bind to Ca+ and Mg- (NO ANTACIDS, DAIRY PRODUCTS, IRON)
-Nursing care: take with 6 to oz of fluid, avoid milk products, iron supplements, antacids, and the sun

-large
-broad spectrum
-use: upper respiratory and lower resp. tract infection, strep throat
-Adverse effects: GI, many drug interactions
-EX: erythromycin
-NOT CONTRAINDICATED WITH MILK
-Nursig Care: take with a meal or snack to avoid GI upset

-narrow spectrum (gm-)
-derived from strep
-rarely oral due to poor absorption
-use: serious life-threatening infections
-ADVERSE EFFECTS: NEPHROTOXIC AND OTOTOXIC
-not used much anymore because better drugs are available
-Nursing Care: monitor peak and trough levels and BUN and serum creatinine levels

-broad spectrum
-bacteriostatic or cidal
-VERY TOXIC!!!! (high association with c diff)
-use: bone, abdominal infections (life-threatening)
-does not cross BBB

-only used in severe infections
-crossed BBB
-ADVERSE EFFECTS: SEVERE BONE DEPRESSION AND GRAY BABY SYNDROME IN NEWBORNS
-Nursing Care: DONT GO IN SUN

-developed for MDR gm + orangisms (very specific infections)
-bacteriostatic

-newest and also only for super bugs
-bactericidal
-need central line

DNA Synthesis Inhbitors

-four generations (first narrow spectrum fro gm - and used ONLY for UTI; 2nd-4th are wider spectrum)
-bactericidal
-use: resp, GI, anthrax
-well absorbed in GI and only qd or bid dosing
-adverse effects: risk of tendon rupture, photosensitivity, NOT WITH ANTACIDS, MILK/DAIRY, VITAMINS, MINERALS
Nursing Care: intake of dairy, vitamins, minerals, antacids should be minimal; avoid the sun, achilles tendon rupture

Antimetabolites (sulfonamides)

-old so lots of bacterial resistance
-use: UTI, ear infection
-Adverse effects: GI, photosensitivity, common cause of allergic reaction, crystaluria, highly protein bound and may displace other protein bound drugs
-Nursing Care: avoid sunlight and tannign beds, birth control decreases, and take with food or milk if PO

Antivirals

-innumocompromised patients (AIDS, HIV, cancer patients, transplant patients)

-Antiviral agents (non HIV)
-Antiretroviral agents (only for HIV/AIDS)

-Block enzyme necessary for symthesis of new viruses so virus can not replicate
-Adverse effects: vary with drug, generally well tolerated and safe

-act by blocking different phase of the replication cycle
-use HAART therapy (drugs from four different categories to treat)

-nucleotide/nucleoside reverse transcriptase inhibitors (NRTI): in DNA and blocks enzyme
-nonnucleosides reverse transcriptase inhibitors (NNRTI): bonds directly to enzyme to inhibit it
-Protease inhibitors (PI's): work in last stage of replication so virus isnt released from CD4 cell
-Fusion inhibitor (newest): WORKS OUTSIDE THE CD4 CELL to stop the c=virus from entering
-Integrase Inhibitors: work inside the cell to integrate and prevent HIV DNA from entering healthy cell DNA

Antifungals
-Topical agents most common
-small group of drugs because fungal infections are hard to kill
-usually require prolonged therapy

-Candida (yeast): mucous membranes
-Dermatophytes: skin, hair, and nails (ex. ringworm, onchomycosis)

-polyenes
-imidazoles or "azoles"
-antimetabolite flucytosine
-echinocadins (newest)
-others (allylamine and griseofulvin)

-DOC for most systemic mycoses
-6-8 weeks of therapy
-very toxic ("shake and bake", nephrotoxic in 80%, ototoxic)
-only given slowly IV
-may pretreat with ASA or benadryl
-black box warning for use only in life threatening infections

-only for candida
-no systemic absorption so no SE(sometimes ordered swish and swallow)
-DOC for chemo related candida

-most commonly used
-can be used systemically or superficially
-all interfere with ergosterol
-most 'azoles' have lots of drug reations
-Ketaconazole is hepatotoxic--alternative to amphotericin B

-interrupts RNA and protein synthesis of fungus
-bone marrow suppression (not used alot now)

-cancidas given slow IV and metabolized by liver
-anidulafungin is not metabolized by the liver (no DRUG INTERACTIONS)
-best safety profile of all drugs in this group
-phlebitis risk---give central line

-not for systemic
-treatment of onychomycosis

-treatment of superficial dermatophyte infections
-product of penicillin
-not for systemic use

-tinactin
-desenex
-lamisil

-mycobacterium tuberculosis bacteria
-affects 1/3 of the world population
-carried by droplets from infected person to host
-located in the lungs
-drug resistance is a HUGE problem (MDR-TB)...why?...No COMPLIANCE IS HIGH
-duration of treatment varies

-Inhibit pprotein synthesis
-inhibit cell wall synthesis
-other
-mot people with TB will be on 2 to 3 different antibiotics (ususllay 1 or 2 primary with 1 or 2 secondary)

-Isoniazid (INH): used alone or in combinations (MOST COMMONLY USED)
-Rifampin
-others

-DOC due to efficacy, low toxicity, and affordability
-bacteriocidal to actively dividing bacilli and bacteriostatic to dormant bacilli
-used alone in prevention and in combination for treatment
-Adverse effects: peripheral neuropathy-prevent with concurrent B6 and HEPATOXICITY (esp. with alcohol or rifampin)

-bancteriocidal
-always in combination due to high risk for resistance
-also DOC in Hansen's Disease
-STAINS BODY FLUIDS RED-ORANGE

-used in combination
-only used in TB
-used if resistant to INH and rifampin
-opti-neuritis (must have eye exam to be put on it)

-usually less effective and more toxic
-used in combination with first line agents

Endoparasitic Infection

Ectoparasitic infections

Antimalarial agents

-affect parasite during the sexual cycle
-The "quines"

-quinine
-causes severe diarrhea and cinchonism (halluncinations)
-used for years but now out due to resistance

-metronidazole
-binds to DNA
-many parasitic infections have a specific drugs used for it

-lindane: (NEUROTOXIC to INFANTS) not indicated for children under 2
-permethrin: safer and made from mums
-THESE ARE BUG KILLERS BE SURE TO FOLLOW INSTRUCTIONS

Antihelmintics

-some are specific for a particular worm so need to ID worm
-mebendazole (Vermox): DOC for most intestinal worms
-invermectin: treat nematodes and heartworms in dogs, along with scabies
-short course of therapy (1 to 3 days) so SE rare

-four antiseptics only used fo UTI
-Nalidixic acid (Negram): 1st generation fluoroquinolone (risk for shoulder tendon rupture)
-Cinoxacin: same as nalidixic acid
-Methenamine: only for chronic UTI
-Nitrofurantion: most serious SE is neuropathy, broad spectrum

-meds applied to the skin
-Antibacterial and antiinfectives
-acne agents
-antifungal
-antivirals for herpes simplex 1 and 2
-topical anesthetics
-pediculicides and scabicides

-drain is plugged
-gradual
-chronic

-occludes drain
-emergency

-beta blockers: nonselective and beta-1 selective DONT AFFECT PUPIL but lower pressure by reducing production of aqueous humor
-Alpha 2 agonists: decrease aqueous humor formation
-prostaglandin analogs: increases drainage of aqueous humor (increase fluid flow)

-change pupil
-parasympathomimetics: Increase outflow through trabecular network; miotics
-carbonic anhydrase inhibitors: diuretic that blocks enzyme involved in production of aqueous humor
-nonselective adrenergics: dilate pupil, decreases rate of production and increase outflow, causes conjuctival pigmentation

-osmotic diuretics: pull fluid from eye and pressure decreases

-antibacterial and antifungal
-antibiotic and steroid combinations
-local anesthetics
-cerumenolytics

agents used to reduce the risk of nosocomial infection

-antiseptics

disinfectants