Pharm One Liners Flashcards
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)
Hepatic metabolism of the drug before it reaches the systemic circulation
First pass effect
The fraction of unchanged drug that reaches systemic circulation after administration
Bioavailability (F)
When the rate of drug input equals the rate of drug elimination
Steady state
Different steps of Phase I
Oxidation, reduction, hydrolysis
Name 3 Phase II conjugation reactions
Glucuronidation, acetylation, glutathione conjugation, glycine conjugation, sulfation, methylation, water conjugation
Constant percentage of drug metabolized per unit time
First order kinetics
Constant amount of drug metabolized per unit time
Zero order kinetics
Target plasma concentration times (volume of distribution divided by bioavailability)
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 biologic effect compared with another drug
Potency
Ability of a drug to produce maximal response after binding to the receptor
Full agonist
Ability to produce less than maximal response after binding to the receptor
Partial agonist
Ability to bind reversibly to the same site as the drug and without activating the effector system
Competitive antagonist
Ability to bind irreversibly to the active site or bind to a site distinctly separate from the agonist binding site
Noncompetitive antagonist
Mechanism of action utilizes ligand gated ion channels
Acetylcholine, nicotine
Dose that produces therapeutic response in 50% of the population
ED50
Dose that is toxic to 50% of the population
TD50
Dose that is lethal to 50% of the population
LD50
Window between therapeutic effect and toxic effect
Therapeutic index
Drugs that have a high margin of safety is indicated by
High therapeutic index
Drugs that have a narrow margin of safety is indicated by
Low therapeutic index
Antidote for lead poisoning
Edetate calcium disodium, succimer, or dimercaprol
Antidote for cyanide poisoning
Nitrates, thiosulfate, hydroxocobalamin
Antidotefor anticholinergic poisoning
Physostigmine
Antidote for iron salt poisoning
Deferoxamine
Antidote for arsenic, mercury, and gold poisoning
Dimercaprol, succimer
Antidote for Wilson’s disease (copper poisoning)
Penicillamine
Antidote for methanol and ethylene glycol toxicity
Fomepizole, ethanol
Antidote for tricyclic antidepressants (TCA)
Sodium bicarbonate (alkalinize plasma)
Antidote for carbon monoxide poisoning
100% O2 and hyperbaric O2
Antidote for digitalis toxicity
Digibind
Antidote for beta-blocker overdose
Glucagon
Method to reduce salicylate intoxication
Sodium bicarbonate (alkalinize urine), dialysis
Muscarinic that is very lipid soluble and used in glaucoma
Pilocarpine
Muscarinic used to treat dry mouth in Sjögren’s syndrome
Pilocarpine or Cevimeline
Cholinesterase inhibitor, short duration of action, used in diagnosis of myasthenia gravis
Edrophonium
Cholinesterase inhibitor, intermediate duration of action, used off-label for postoperative paralytic ileus and urinary retention
Neostigmine
Cholinesterase inhibitor, lipid soluble, indicated for atropine overdose and glaucoma
Physostigmine
Treatment of myasthenia gravis and sometimes used prophylactically for organophosphate poisoning in chemical warfare
Pyridostigmine
Organophosphate, indicated for glaucoma but not used much clinically due to long duration of action
Echothiophate
Insecticide organophosphate
Malathion, parathion
The most important cause of acute deaths in cholinesterase inhibitor toxicity
Respiratory failure
Used in treatment of muscarinic symptoms in organophosphate overdose
Atropine
Mechanism of action of atropine
Nonselective antimuscarinic
Antimuscarinic indicated for overactive bladder muscle dysfunction
Oxybutynin
Toxicity of anticholinergics
Anti-DUMBBELSS
Another pneumonic for anticholinergic toxicity
“dry as a bone, red as a beet, mad as a hatter, hot as a hare, blind as a bat”
Atropine fever is the most dangerous effect and can be lethal in this population group
Infants
Contraindications to use of atropine
Infants, closed angle glaucoma, prostatic hypertrophy
Pneumonic for beta receptors
You have 1 heart (Beta 1) and 2 lungs (Beta 2)
Drug of choice for anaphylactic shock
Epinephrine
Indirect acting sympathomimetic, reuptake inhibitor, commonly abused, indicated for attention deficit disorder and weight reduction
Methamphetamine
Alpha agonist indicated for nasal congestion, hypotension, and mydriasis induction
Phenylephrine
Short acting beta 2 agonist, drug of choice for acute asthma
Albuterol
Longer acting beta 2 agonist, indicated for prophylaxis of asthma
Salmeterol
Its ability to increase heart rate makes it useful as adjunct therapy for acute heart failure and hypovolemia or septic shock
Beta 1 agonist
Indicated for symptomatic orthostatic hypotension
Midodrine
Beta 2 agonist used to suppress premature labor, but cardiac stimulatory effects may be hazardous to mother and fetus
Terbutaline
Indirect acting sympathomimetic, improves urinary continence in children and elderly with enuresis
Ephedrine
Beta agonists used in acute congestive heart failure
Dobutamine and dopamine
Beta 1 agonist toxicity
Sinus tachycardia and serious arrhythmias
Beta 2 agonist toxicity
Skeletal muscle tremor
Irreversible, nonselective alpha-blocker indicated for pheochromocytoma
Phenoxybenzamine
Reversible, nonselective alpha blocker indicated for pheochromocytoma
Phentolamine
Blocks alpha 1 and beta receptors and indicated for the treatment of CHF
Labetalol and carvedilol
Beta blockers with partial agonist activity, can bronchodilate and may have an advantage treating patients with asthma
Pindolol and acebutolol
Short-acting beta blocker that can be given parenterally
Esmolol
Clinical uses of these agents include treatment of hypertension, angina, arrhythmias, and chronic congestive heart failure
Beta blockers
Beta-blockers should be used cautiously in
Asthma (bronchospastic effects), diabetes (block signs of hypoglycemia) and peripheral vascular disease
Beta blockers are used for this type of angina attack
Classic (exertional) angina
A nonselective beta blocker with alpha 1 blocking effect indicated for congestive heart failure
Carvedilol
This class of drugs inhibit angiotensin-converting enzyme
ACE inhibitors
Mechanism of action of calcium channel blockers
Block L-type calcium channels
Side effects of methyldopa
Positive Comb’s hemolytic anemia, SLE-like syndrome, CNS depression
Side effect of clonidine
Rebound hypertension, sedation, dry mouth
Direct vasodilator of arteriolar smooth muscle by increasing cGMP and inhibit IP3-induced calcium release from the sarcoplasmic reticulum
Hydralazine
Arterial vasodilator that works by opening K+ channels
Minoxidil
Side effect of minoxidil
Hypertrichosis
IV nitrate used in hypertensive crisis
Nitroprusside
Nitroprusside vasodilates
Arteries and veins
Side effect of nitroprusside
Cyanide poisoning
Drugs used in the management of exertional (classic) angina
Nitrates, calcium channel blockers, beta blockers
Aspirin reduces mortality in unstable angina by
Inhibiting platelet aggregation
Nitrate free intervals are needed due to
Tolerance
Side effects of nitrates
Reflex tachycardia, hypotension, flushing, and throbbing headache due to meningeal artery dilation
Mechanism of action of cardiac glycosides (eg. digoxin)
Inhibit Na+/K+ ATPase and indirectly increase intracellular calcium and cardiac contractility
Indication of digoxin
Atrial fibrillation and congestive heart failure
Digoxin toxicity can be precipitated by
Hypokalemia
Phosphodiesterase (PDE3) inhibitors indicated for acute congestive heart failure; long term use is associated with increased mortality
Amrinone and milrinone
Side effect of amrinone and milrinone
Thrombocytopenia
Agent used in acutely decompensated congestive heart failure resembling natriuretic peptide
Nesiritide
Mechanism of action of class II antiarrhythmics
Beta -blockers
Mechanism of action of class IV antiarrhythmics
Calcium channel blockers
Major drug interaction with quinidine
Increases concentration of digoxin
Contraindication of disopyramide use
Heart failure
Used as last line antiarrhythmic agents due to proarrhythmic property; strongest sodium channel blocker
Class IC (flecainide, propafenone)
Anti-arrhythmic agents that decrease mortality
B-blockers
Used intravenously for acute tachycardia during and post- surgery
Esmolol
Antiarrhythmic effective in most types of arrhythmia
Amiodarone
Class III antiarrhythmic that exhibits properties of all 4 classes
Amiodarone
Antiarrhythmic that exhibits Class II and III properties
Sotalol
Side effect of sotalol
prolongs QT interval
Drug of choice for narrow complex paroxysmal supraventricular tachycardia (PSVT)
Adenosine
Mechanism of action of adenosine
Activates G-protein coupled K+ channels in atrium, SA and AV node
Anti-arrhythmic with <10 second duration of action
Adenosine
Drug of choice for early after depolarizations (Torsade)
Magnesium sulfate
HMG CoA reductase inhibitors are contraindicated in
Pregnancy
Concurrent use of fibrates and statins increases risk of
Rhabdomyolysis
Class of agents for cholestyramine, colestipol, colesevalem
Bile acid-binding resins
Major nutritional side effect of bile acid-binding resins
Impair absorption of fat soluble vitamins (A,D,E,K)
Side effect of fenofibrate and gemfibrozil
Gallstone formation
Cutaneous flush due to niacin can be reduced by pretreatment with
NSAIDs
Inhibits intestinal cholesterol absorption by inhibiting Niemann Pick C1 Like 1 (NPC1L1) Protein
Ezetimibe
Mechanism of action of aspirin
Irreversibly blocks COX1 and COX2
Agent used to treat myocardial infarction (MI) and to reduce incidence of subsequent MI
Aspirin
Antiplatelet drug reserved for patients allergic to aspirin
Ticlopidine
Side effect for ticlopidine
Neutropenia and agranulocytosis
Irreversible inhibitor of platelet P2Y12 receptors; effective in preventing transient ischemic attack
Clopidogrel and ticlopidine
Phosphodiesterase inhibitor indicated for intermittent claudication
Dipyridamole, cilostazol
Block glycoprotein IIb/IIIa involved in platelet cross-linking
Abciximab, tirofiban and eptifibatide
Route of administration of warfarin
Oral
Contraindication of warfarin
Pregnancy
Anticoagulant of choice in pregnancy
Heparin
Routes of administration of heparin
IV and SC
Side effect of both warfarin and heparin
Bleeding
Two anticoagulant used for prophylaxis and treatment of thrombosis in patients with heparin-induced thrombocytopenia
Bivalirudin, argatroban
Thrombolytic used for acute myocardial infarction and ischemic (non-hemorrhagic) cerebral vascular accident (stroke)
Alteplase
Side effect of tissue plasminogen activators
cerebral hemorrhage
Thrombolytic that can cause allergic reaction and non-selective systemic fibrinolysis
Streptokinase
Carbonic anhydrase inhibitor
Acetazolamide
Mechanism of action of loop diuretics
inhibits Na+/K+/2Cl- cotransporter
Diuretic used in hypertensive patients with renal failure
Loop diuretics (furosemide, ethacrynic acid, butmetanide)
Aminoglycosides used with loop diuretics potentiate this adverse effect
Ototoxicity
Mechanism of action of thiazide diuretics
Inhibit Na+/Cl- cotransport
Diuretic used as first line for treatment of hypertension
Thiazides
Class of drugs that may cause cross-sensitivity with thiazide diuretics
Sulfonamides
Mechanism of action of spironolactone
Inhibit mineralocorticoid (aldosterone) receptor resulting in inhibition of Na/K-ATPase and ENaC synthesis
Diuretics work in congestive failure by
Reducing preload
Agents used for syndrome of inappropriate antidiuretic hormone (SIADH) secretion
Tolvaptan and conivaptan
An early generation tetracycline that may be used for chronic persistant syndrome of inappropriate antidiuretic hormone (SIADH) secretion
demeclocycline
Side effect of demeclocycline
Stunted bone growth and teeth discoloration for children under 8 years of age
Antibacterials for optimal treatment of acute uncomplicated cystitis
Nitrofurantoin, trimethoprim-sulfamethoxazole, fosfomycin
Antibacterials for optimal treatment of acute pyelonephritis
Fluoroquinolones (ciprofloxacin, levofloxacin), trimethoprim-sulfamethoxazole
Mechanism of action of penicillin
Block cell wall synthesis by inhibiting transpeptidase and block peptidoglycan cross-linkage
Penicillins active against penicillinase secreting bacteria
Methicillin, nafcillin, and dicloxacillin
Class of antibiotics that have 10% cross sensitivity with penicillins
Cephalosporins
Penicillins active against pseudomonas
Piperacillin and ticarcillin
Beta lactam that can be used in penicillin-allergic patients
Aztreonam
Side effect of imipenem
Seizures
Drug of choice for treatment of serious pseudomembranous colitis
Oral vancomycin
Antibiotic causing red-man syndrome, and prevention
Vancomycin, can be prevented by infusion
at a slow rate and antihistamines
Drug causes teeth discoloration
Tetracycline
Mechanism of action of tetracycline
Decreases protein synthesis by binding to 30S ribosome and prevent binding of tRNA
Two toxicities of aminoglycosides
Nephro and ototoxicity
Aminoglycoside less used due to its irreversible vestibular toxicity
Streptomycin
Mechanism of action of macrolides (erythromycin, clarithromycin)
Inhibit protein synthesis by binding to 23S rRNA of 50S ribosome subunit
Drug of choice for Legionnaires’ disease
Azithromycin or levofloxacin
Drug notorious for causing pseudomembranous colitis
Clindamycin
Drug that causes gray baby syndrome and aplastic anemia
Chloramphenicol
Inhibits isoleucyl tRNA and used topically for impetigo
Mupirocin
Side effect of metronidazole when given with alcohol
Disulfiram-like reaction
Neurotoxicity with isoniazid can be prevented by
Administration of Vit B6 (pyridoxine)
Side effect of isoniazid
Systemic lupus erythematosus, peripheral neuritis, hepatitis
Drug of choice for leprosy
Dapsone
Toxicity of amphotericin
Nephrotoxicity
Side effect of ketoconazole only in men
Gynecomastia
Mechanism of action of nystatin
Binds to ergosterol and creates a pore in fungal membrane
Drug used in exoerythrocytic cycle of malaria
Primaquine
Drug of choice for cytomegalovirus (CMV) treatment
Ganciclovir