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20 Cards in this Set
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Abatacept
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Class
Selective costimulation modulator inhibiting the costimulation of T cells Indications Treatment of rheumatoid arthritis in the case of inadequate response to anti-TNFα therapy psoriasis Administration/Absorption Dosage Distribution Mechanism Fusion protein composed of an immunoglobulin fused to the extracellular domain of CTLA-4, which can bind B7 Binding to the B7 protein on APCs prevents them from delivering the costimulatory signal to T cells Thus prevents the full activation of T cells.[1][2] Excretion Side effects Interactions Contraindications |
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Abciximab
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Indications
prevention of ischaemic cardiac complications in patients undergoing percutaneous coronary intervention short-term prevention of myocardial infarction in patients with unstable angina not responding to conventional treatment and who are scheduled for percutaneous coronary intervention Administration/Absorption IV injection/infusion Dosage initially by intravenous injection over 1 minute, 250 micrograms/kg, then by intravenous infusion, 125 nanograms/kg/minute (max. 10 micrograms/minute) Distribution Mechanism platelet aggregation inhibitor glycoprotein IIb/IIIa receptor antagonist Excretion plasma half life of about ten minutes, with a second phase half life of about 30 minutes but due to its strong affinity for its receptor on the platelets, it may occupy some receptors for weeks Side effects bleeding manifestations; nausea, vomiting, hypotension, bradycardia, chest pain, back pain, headache, fever, puncture site pain, thrombocytopenia rarely cardiac tamponade, adult respiratory distress, hypersensitivity reactions Interactions Contraindications |
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Acetazolamide
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Class
carbonic anhydrase inhibitor Indications glaucoma epileptic seizures benign intracranial hypertension (pseudotumor cerebri) altitude sickness cystinuria dural ectasia Administration/Absorption Dosage Distribution Mechanism Prevents H2CO3 conversion to CO2 + H2O in kidney tubules CO2 normally rapidly diffuses into blood This is the mechanism of HCO3- reabsorption in the kidney H2CO3 therefore leaves in the urine H+ taken up with Cl- => hyperchloremic metabolic acidosis Excretion Side effects Interactions Contraindications |
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Adalimumab
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Class
TNF inhibitor Indications rheumatoid arthritis psoriatic arthritis ankylosing spondylitis Crohn's disease moderate to severe chronic psoriasis juvenile idiopathic arthritis Administration/Absorption subcut injection Dosage Distribution Mechanism binds to TNFα, preventing it from activating TNF receptors constructed from a fully human monoclonal antibody Excretion Side effects Reactivation of latent infections such as tuberculoses Immune system may be unable to fight new infections Interactions Contraindications |
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Aledronate
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Class
Bisphosphonate Indications Treatment and prevention of osteoporosis in women Paget's disease of bone To reduce hypercalcemia in tumor-induced bone disease Administration/Absorption Mean oral bioavailability of alendronate in women was 0.7% Dosage Prophylaxis of osteoporosis in women: 5–10 mg daily or 35–70 mg weekly Paget's Disease: 40 mg daily for 6 months Distribution 78% protein bound VOD 28 L Mechanism Based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone Also targets farnesyl pyrophosphate (FPP) synthase Acts as a analogue of isoprenoid diphosphate lipids, thereby inhibiting FPP synthase An enzyme in the mevalonate pathway Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) Essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins This activity inhibits osteoclast activity and reduces bone resorption and turnover Excretion There is no evidence that alendronate is metabolized in humans or animals Approximately 50% excreted in the urine within 72 hours Side effects Can damage the esophagus By toxicity from the medication itself Also by nonspecific irritation secondary to contact between the pill and the esophageal mucosa Rash Osteonecrosis of the Jaw Rare instances of auditory hallucinations and visual disturbances Interactions Milk, diet, and drugs containing high amounts of calcium, magnesium or aluminium decrease absorption The combination of NSAIDs and alendronate may increase the risk of gastric ulcers Contraindications Acute inflammations of the gastrointestinal tract (esophagitis, gastritis, ulcerations) Clinically manifest osteomalacia Certain malformations and malfunctions of the esophagus (strictures, achalasia) Inability to stand, walk, or sit for 30 minutes after oral administration Renal impairment with a creatinine clearance below 30ml/min Hypersensitivity to alendronate or another ingredient Hypocalcemia Pregnancy and breastfeeding Patients below 18 yrs. of age, as no clinical data exists |
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Alteplase
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Indications
Thrombolysis myocardial infarction with ST-elevation (STEMI) acute ischemic stroke (AIS) acute massive pulmonary embolism central venous access devices (CVAD) Administration/Absorption Distribution Mechanism Recombinant tissue plaminogen activator catalyzes the conversion of plasminogen into plasmin by cleaving the single-chain plasminogen into two chains These two chains are linked by a disulfide bond and the resulting molecule is called plasmin. Excretion Side effects |
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Amiloride
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Class
Potassium-sparing diuretic Indications hypertension congestive heart failure. Administration/Absorption Dosage Distribution Mechanism Directly blocks the epithelial sodium channel (ENaC) thereby inhibiting sodium reabsorption in the late distal convoluted tubules, connecting tubules, and collecting ducts Promotes the loss of sodium and water from the body, but without depleting potassium Excretion Side effects Interactions Contraindications |
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Amiodarone
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Indications
antiarrhythmic agent various types of tachyarrhythmias both ventricular and supraventricular (atrial) arrhythmias Administration/Absorption Distribution Mechanism class III antiarrhythmic agent prolongs phase 3 of the cardiac action potential beta blocker-like and potassium channel blocker-like actions on the SA and AV nodes increases the refractory period via sodium- and potassium-channel effects slows intra-cardiac conduction of the cardiac action potential, via sodium-channel effects Excretion |
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Amlodipine
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Indications
anti-hypertensive angina Administration/Absorption Distribution Mechanism long-acting calcium channel blocker dihydropyridine class inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle Binds to both dihydropyridine and nondihydropyridine binding sites. Excretion |
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Aripiprazole
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Class
Benzisoxazole derivative atypical antipsychotic Indications schizophrenia bipolar disorder clinical depression Administration/Absorption Oral IM Dosage Distribution VOD 4.9 L/kg Mechanism Dopamine normaliser Stimulates if levels low Inhibits if levels high Selective monoaminergic antagonist with high affinity for: Serotonin Type 2 (5HT2) Dopamine Type 2 (D2) 1 and 2 adrenergic H1 histaminergic Aripiprazole's antipsychotic activity is likely due to a combination of antagonism at: D2 receptors in the mesolimbic pathway 5HT2A receptors in the frontal cortex Antagonism at D2 receptors relieves positive symptoms while antagonism at 5HT2A receptors relieves negative symptoms of schizophrenia Excretion Hepatic metabolism Urine / faeces Halflife 75-146 hours Side effects akathisia headache agitation anxiety unusual tiredness or weakness nausea and vomiting an uncomfortable feeling in the stomach constipation increased production of saliva light-headedness insomnia sleepiness shaking blurred vision sexual dysfunction Interactions Contraindications |
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Aspirin
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Indications
Headache Pain Prevention of heart attacks and strokes Coronary and carotid arteries, bypasses and stents Dosage Acute MI 300 mg sublingually Prophylactic 40-75 mg Administration/Absorption Oral Distribution 50–80% of salicylate in the blood is bound by protein Mechanism Irreversible inactivation of the cyclooxygenase (PTGS - prostaglandin-endoperoxide synthase) enzyme acts as an acetylating agent where an acetyl group is covalently attached to a serine residue in the active site of the PTGS enzyme Irreversibly blocks the formation of thromboxane A2 in platelets, producing an inhibitory effect on platelet aggregation Activated platelets release the contents of stored granules into the blood plasma, which activate further platelets The granules include ADP, serotonin, platelet-activating factor (PAF), vWF, platelet factor 4, and thromboxane A2 (TXA2) 40 mg of aspirin a day is able to inhibit a large proportion of maximum thromboxane A2 release provoked acutely, with the prostaglandin I2 synthesis being little affected Excretion Side effects Reye's syndrome GI bleeds Interactions Contraindications |
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Atenolol
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Indications
hypertension coronary heart disease arrhythmias angina post-myocardial infarction Graves Disease, until antithyroid medication can take effect Administration/Absorption Distribution Unlike propranolol, atenolol does not pass through the blood-brain barrier thus avoiding various central nervous system side effects. Mechanism selective β1 receptor antagonist Excretion tcmax = 2 to 4 hours after oral dosing mean elimination halflife is 6 hours |
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Baclofen
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Class
GABAB receptor agonist Indications Spasticity Potentially.. alcoholism TLESR Administration/Absorption Rapidly absorbed after oral administration Dosage Distribution Widely distributed throughout the body Mechanism Excretion Side effects Interactions Contraindications |
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Beclometasone
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Indications
prophylaxis of asthma rhinitis sinusitis Unusually severe aphthous ulcers eczema Administration/Absorption Distribution Mechanism glucocorticoid steroid Excretion Side effects cough upon inhalation oral candidiasis unpleasant taste hoarseness or nasal congestion pain or headache visual changes |
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Bendroflumethiazide
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Indications
hypertension mild heart failure familial hyperkalemia edema urinary tract disorders Dosage Administration/Absorption Absorbed relatively rapidly after oral administration Distribution 96% protein bound Mechanism Thiazide diuretic Inhibits Na+/Cl- reabsorption at the beginning of the distal convoluted tubule (DCT) by blocking the thiazide-sensitive Na-Cl cotransporter => Excretion of sodium, chloride and water This results in an increase in potassium excretion via the sodium-potassium exchange mechanism Vasodilation Mechanism unclear Activating calcium-activated potassium channels (large conductance) in vascular smooth muscles? Inhibiting various carbonic anhydrases in vascular tissue? Thiazides also cause an increase in serum uric acid Excretion Half life 8.5 hrs Side effects Common adverse effects postural hypotension hyponatraemia, hypokalaemia, hypercalcaemia gout impaired glucose tolerance impotence Rare adverse effects thrombocytopenia agranulocytosis photosensitivity rash pancreatitis Interactions Contraindications |
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Benzylpenicillin
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Indications
Cellulitis Bacterial endocarditis Gonorrhea Meningitis Aspiration pneumonia, lung abscess Community-acquired pneumonia Syphilis Septicemia in children Septic Arthritis Administration/Absorption parenteral Dosage Distribution Mechanism Inhibits the formation of peptidoglycan cross-links in the bacterial cell wall The β-lactam moiety (functional group) of penicillin binds to the enzyme (DD-transpeptidase) that links the peptidoglycan molecules in bacteria. The enzymes that hydrolyze the peptidoglycan cross-links continue to function, which weakens the cell wall of the bacterium In addition, the build-up of peptidoglycan precursors triggers the activation of bacterial cell wall hydrolases and autolysins, which further digest the bacteria's existing peptidoglycan Shows a synergistic effect with aminoglycosides inhibition of peptidoglycan synthesis allows aminoglycosides to penetrate the bacterial cell wall more easily, allowing its disruption of bacterial protein synthesis within the cell This results in a lowered MBC for susceptible organisms. Excretion Side effects Interactions Contraindications |
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Betamethasone
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Indications
skin irritation, such as itching and flaking from eczema psoriasis phimosis Stimulation of fetal lung maturation (prevention of IRDS) Administration/Absorption topical cream, ointment, foam, lotion or gel to treat itching IM IV Dosage Distribution Mechanism moderately potent glucocorticoid steroid anti-inflammatory and immunosuppressive properties Excretion Side effects hypoglycemia and leukocytosis in newborns exposed in utero. Interactions Contraindications |
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Bethanecol
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Indications
Urinary retention resulting from general anesthetic or diabetic neuropathy of the bladder Gastrointestinal atony Administration/Absorption orally or subcutaneously Distribution Mechanism Parasympathomimetic choline ester selectively stimulates muscarinic receptors without any effect on nicotinic receptors Unlike acetylcholine, bethanechol is not hydrolyzed by cholinesterase and will therefore have a long duration of action Bethanechol does not involve the action of the muscarinic M3 receptor subtype in-vitro Excretion |
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Captopril
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Indications
Hypertension Cardiac conditions such as post myocardial infarction and congestive heart failure Preservation of kidney function in diabetic nephropathy Administration/Absorption Distribution Mechanism Angiotensin-converting enzyme inhibitor Excretion |
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Carbachol
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Indications
glaucoma Administration/Absorption topical ocular or through intraocular injection two to 5 minute onset of action and its duration of action is 4 to 8 hours with topical administration and 24 hours for intraocular administration Distribution Mechanism cholinergic agonist Binds and activates the acetylcholine receptor parasympathomimetic that stimulates both muscarinic and nicotinic receptors In topical ocular and intraocular administration its principal effects are miosis and increased aqueous humour outflow. Excretion not easily metabolized by cholinesterase |
