(First Aid) Pharmacology – Flashcards
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Measures the affinity of an enzyme for its substrate ( dec Km = inc affinity)
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Km
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Maximal velocity of an enzymatic reaction (proportional to enzyme concentration)
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Vmax
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Does not change Vmax (Lineweaver-Burke lines cross each other "competitively")
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Competitive inhibition
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Decreases Vmax (Lineweaver-Burke lines do not cross each other)
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Noncompetitive inhibition
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Drug in body / plasma drug concentration (low Vd (4-8L: in blood), medium Vd (in extracellular space), High Vd (> body weight: in tissues))
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Volume of Distribution (Vd)
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Rate of elimination of drug / plasma drug concentration (OR Vd x Kc, where Kc is the elimination constant)
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Clearance (CL)
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T1/2 = (0.7 x Vd) / CL
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Half life (t1/2)
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1:50%, 2:75%, 3:87.5%, 4:93.75%
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Concentration of a substance after X half lives (1,2,3,4)
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= Cp x (Vd / F); (Cp: target plasma conc., F: bioavailability, 1 if by IV)
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Loading dose
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= Cp x (CL / F); (Cp: target plasma conc., F: bioavailability, 1 if by IV; a renal patient would have decreased clearance, so they would need a decreased maintenance dose)
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Maintenance dose
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PEA (phenytoin, ethanol, aspirin)
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Common drugs that follow zero-order elimination
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Will get trapped in a basic environment, treat with bicarbonate
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Treating a weak acid overdose
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Will get trapped in an acidic environment, treat with ammonium chloride
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Treating a weak base overdose
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(Cytochrome P450) 1. reduction, 2. oxidation, 3. hydrolysis (drugs became slightly polarized, may still be active)
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Reactions involved in phase I drug metabolism
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(Conjugation) 1. acetylation, 2. glucuronidation, 3. sulfonation (drugs become very polarized, are inactivated)
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Reactions involved in phase II drug metabolism
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Competitive antagonist shifts curve right, requires bigger dose of drug for effect (inc EC50); noncompetitive antagonist shortens curve, cannot reach same level of effect (dec efficacy)
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Effect of competitive antagonists on efficacy curves versus noncompetitive antagonists
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Partial agonists will have a lower maximal efficacy than full agonists (however potency is independent, they may still be more potent or less potent than a full agonist)
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Effect of partial agonists versus full agnoists on efficacy curves
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TILE: TI = LD50 / ED50 (median toxic dose / median effective dose; Safer drugs have HIGHER TI values)
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Therapeutic index (TI)
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Receptor location: NMJ; Function: skeletal muscle contraction; Mechanism: ion channel (Na influx)
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Nm receptors
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Receptor location: Ganglia; Function: stimulates sympathetics and parasympathetics; Mechanism: ion channel (Na influx);
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Nn receptors
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Receptor location: Nerve endings; Function: Gastric acid secretion; Mechanism: Gq protein;
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M1 receptors
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Receptor location: Heart; Function: Inhibitory, reduces heart rate; Mechanism: Gi protein;
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M2 receptors
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Receptor location: Smooth muscle, endothelium, glands; Function: bronchoconstriction, pupil constriction, accommodation, increases secretions; Mechanism: Gq proteins;
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M3 receptors
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Receptor location: Arterioles, glands; Function: vasoconstriction, pupillary dilation; Mechanism: Gq protein;
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α1
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Receptor location: presynaptic nerve endings; Function: inhibitory, feedback inhibition of NT release; Mechanism: Gi protein;
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α2
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Receptor location: heart, kidney; Function: heart stimulation, renin release; Mechanism: Gs protein;
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β1
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Receptor location: lungs, skeletal muscle; Function: Vasodilation, bronchiole dilation, ciliary process (makes aqueous humour); Mechanism: Gs protein;
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β2
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Receptor location: Fat; Function: excitatory; Mechanism: Gs protein;
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β3
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Function: vasodilation; Mechanism: Gs protein;
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D1
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Function: Causes NT release in brain; Mechanism: Gi protein;
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D2
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Function: stimulates mucuous production, bronchiole constriction, pain, itching; Mechanism: Gq protein;
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H1
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Function: gastric acid secretion; Mechanism: Gs protein;
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H2
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Function: vasoconstriction; Mechanism: Gq protein;
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V1
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Function: inc H20 permeability, reabsorption in collecting tubules in kidney; Mechanism: Gs protein;
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V2
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Sick of sex (SIQ, SQS) D1,D2, H1, H2, V1, V2
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Mnemonic for gprotein receptors used for D, H, and V receptors
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Gq protein activates PLC, IP3 + DAG, inc Ca++ (IP3) and activate PKC (DAG)
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Function of Gq protein receptors
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Gi protein activates K+ channels, inhibition of adenylate cyclase, reduction of cAMP
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Function of Gi protein receptors
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Gs protein activates adenylate cyclase, increases cAMP
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Function of Gs protein receptors
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DUMBBELSS (Diarrhea, urination, miosis, bronchospasm, bradycardia, excitation (of skeletal muscle), lacrimation, sweating, salivation); treatment: atropine (reverses symptoms) + pralidoxime (regenerates cholinesterase)
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Symptoms of cholinesterase inhibitor poisoning
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Hot as a hare (inc temp), Dry as a bone (dec secretions), Red as a beet (flushed skin), Blind as a bat (cycloplegia), Mad as a hatter
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Symptoms of muscarinic antagonist overdose
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Bethanechol, carbachol, pilocarpine, methacholine
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Direct cholinergic agonist drugs
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Bethanechol
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Direct cholinergic agonist; activates bowel and bladder post operation
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Carbachol
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Direct cholinergic agonist; used in glaucoma (causes pupillary contraction and reduces ICP)
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Pilocarpine (PILE on the sweat and tears)
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Direct cholinergic agonist; potent stimulator of sweat and tears
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Methacholine
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Direct cholinergic agonist; challenge test for asthma diagnosis
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(-stigmine, Ed PHYSted the MAiLman and it ECHOed) Neostigmine, pyridostigmine, physostigmine, edrophonium, echothiophate, malathion
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Indirect cholinergic agonist drugs (anticholinesterases)
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Neostigmine (NEO CNS)
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Indirect cholinergic agonist; used in post operative reversal of NMJ block; does NOT penetrate the CNS
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Pyridostigmine
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Indirect cholinergic agonist; used for myasthenia gravis (due to it's long action); does NOT penetrate the CNS
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Physostigmine (PHYS is for EYES)
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Indirect cholinergic agonist; Used for glaucoma and atropine overdose (does cross CNS)
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Edrophonium
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Indirect cholinergic agonist; Used to diagnose myasthenia gravis (extremely short action)
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Echothiophate
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Indirect cholinergic agonist; used for glaucoma
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Atropine, homatropine, tropicamide, benztropine, scopolamine, ipratropium, methscopolamine, oxybutynin, glycopyrrolate, pirenzepine, propantheline
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Muscarinic antagonist drugs
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Atropine (or homatropine, tropicamide)
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Muscarinic antagonist drug(s); produces mydriasis and cycloplegia (eye)
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Benztropine (PARK my BENZ)
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Muscarinic antagonist drug; treatment for parkinson's (CNS)
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Scopolamine
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Muscarinic antagonist drug; treatment of motion sickness (CNS)
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Ipratropium
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Muscarinic antagonist drug; treats asthma and COPD (respiratory)
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Methscopolamine (or oxybutynin, glycopyrrolate)
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Muscarinic antagonist drug(s); Reduces bladder urgency in cystitis and bladder spasms (GI)
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Pirenzepine (or propantheline)
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Muscarinic antagonist drug(s); treatment of peptic ulcers (GI)
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Atropine
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Muscarinic antagonist drug; Used to block DUMBBELSS; Toxicity: hot as a hare, dry as a bone, red as a beet, blind as a bat, mad as a hatter
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Hexamethonium
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Nicotinic antagonist; ganglion blocker, used in experimental models to prevent vaga reflex responses to BP changes
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B1
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Low doses of epinephrine are selective for what receptor?
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Epinephrine
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Drug used for anaphylaxis, open angle glaucoma, asthma and hypotension. Binds a1, a2, B1 and B2 receptors.
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Norepinephrine
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Drug used for hypotension. Binds a1, a2 > B1
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Isoproterenol
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Drug that binds B1 = B2. Used rarely for AV block
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Dopamine
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Drug used for shock (by increased renal perfusion), and heart failure. Binds D1 = D2 > B > a.
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Dobutamine
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Drug used for shock, heart failure, and cardiac stress test. Bind B1 > B2.
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Dopamine is inotropic and chronotropic, Dobutamine is inotropic but not chronotropic.
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What is the difference in inotropy and chronotropy between dopamine and dobutamine.
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Phenylephrine.
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Drug used for pupillary dilation, vasoconstriction, and nasal decongestion. Binds a1 > a2.
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Albuterol
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Drugs used for acute asthma. Binds B2>B1/
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Terbutaline
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Drug used to reduce premature uterine contractions. Binds B2 > B1.
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Ritodrine
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Drug used to reduce premature uterine contractions. Binds B2 only.
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Amphetamine
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Drug used to treat narcolepsy, obesity, ADD. Releases stored catecholamines.
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Ephedrine
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Drug used for nasal decongestion, urinary incontinence, and hypotension. Releases stored catecholamines.
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Cocaine
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Drug that causes vasoconstriction and local anesthesia. Inhibits reuptake of NE.
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Clonidine, a-methyldopa
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Drug used to treat hypertension (esp in renal disease because it prevents decrease in blood flow to kidney. Centrally acting a2 agonist.
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Increased systolic and diastolic pressure, reflex bradycardia (all because a>B)
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Effect of NE on systolic and diastolic BP, and heart rate.
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Increased systolic (B1), decreased diastolic (B2) (wide PP, no change in mean BP), increased heart rate (B1)
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Effect of epinephrineon systolic, diastolic BP and heart rate
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Decrease BP (sys and diastolic, B2), BIG increase in HR (B1) (isoproterenol = B > a)
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Effect of isoproterenol on BP and heart rate
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MAST (metaproterenol, albuterol, salmeterol, terbutaline)
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Mnemonic for selective B2 agonists
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Phenoxybenzamine (irreversible), Phentolamine (reversible, both nonselective alpha blockers)
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Drugs (2) used in pheochromocytoma before tumor is removed. SE: orthostatic hypotension, reflex tachycardia
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(a1 antagonists) Prazosin, Terazosin, doxazosin
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Alpha antagonist used for hypertension and urinary retention in BPH. SE: first dose orthostatic hypotension
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(a2 selective) Mirtazapine
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Alpha antagonist used for depression. SE: sedation, inc serum cholesterol, inc appetite.
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Dec CO, dec renin secretion (B1)
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How do beta blockers effect hypertension
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Dec mortality after MI
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How are B blockers used in MI
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Propanolol, esmolol
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What B blockers are used in supraventricular tachycardia
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Dec. AV conduction velocity (SVT)
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What type of arrhythmia are B blockers used for
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Dec secretion of aqueous humor (timolol)
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How are B blockers used in glaucoma.
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Impotence, exacerbates asthma, don't use with diabetics
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What are the sideeffects of B blockers
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Propanolol, timolol, nadolol, pindolol, labetalol
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What are the nonselective B blockers
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A BEAM of B1 blockers (acebutolol, betaxolol, esmolol, atenolol, metoprolol)
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What are the selective B1 blockers (mnemonic)
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Carvedilol, labetalol
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Nonselective alpha and beta antagonists
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N-acetylcysteine
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Treatment for overdose of acetominophen
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NaHCO3 (alkalinize urine), dialysis
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Treatment for overdose of Salicylates
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NH4Cl (acidify urine)
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Treatment for overdose of amphetamines
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Atropine, pralidoxime
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Treatment for overdose of anticholinesterases, organophosphates
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Physostigmine saligylate
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Treatment for overdose of antimuscainic and anticholinergic agents
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Glucagon
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Treatment for overdose of B blockers
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K+, lidocaine, digibind, Mg2+
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Treatment for overdose of digitalis
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Deferoxamine
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Treatment for overdose of iron
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CaEDTA, dimercaprol, succimer (kids), penicilamine
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Treatment for overdose of lead
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Dimercapol, succimer
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Treatment for overdose of arsenic, mercury, gold
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Penicillamine
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Treatment for overdose of copper, arsenic, gold
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Nitrite, hydroxycobalamin, thiosulfate
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Treatment for overdose of cyanide
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Methylene blue
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Treatment for overdose of methemoglobin
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100% O2, hyperbaric O2
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Treatment for overdose of CO
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Ehtanol, dialysis, fomezipol
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Treatment for overdose of methanol or ethylene glycol (antifreeze)
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Naloxone, naltrexone
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Treatment for overdose of opiods
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Flumazenil
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Treatment for overdose of benzodiazapines
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NaHCO3 (serum alkanization)
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Treatment for overdose of TCAs
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Protamine
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Treatment for overdose of heparin
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Vitamin K, fresh frozen plasma
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Treatment for overdose of warfarin
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Aminocaproic acid
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Treatment for overdose of tPA, streptokinase
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Lead poisining
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Sx: lines on gingivae and long bone epiphyses, encephalopathy and erythrocyte basophilic stippling, abdominal colic, sideroblastic anemia, wrist and foot drop
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Iron poisining
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Acute poisining = gastric bleeding, chronic poisining = metaboic acidosis, GI obstruction (scarring). MOA = peroxidation of lipids
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Tricyclics
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What drugs give an atropine like side effect to the cardiovascular system?
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Cocaine, sumatripan
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What drugs (2) cause coronary vasospasm as a side effect?
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Niacin, Ca channel blockers, adenosine, vancomycin
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What drugs (4) cause cutaneous flushing as a side effect
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Doxorubicin, daunorubicin
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What drugs (2) cause dilated cardiomyopathy as a side effect
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Class III antiarrythmics (sotalol), Class IA (quinidine) antiarrhythmics, cisapride
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What drugs (3) cause torsades de pointes as a side effect
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Clozapine, carbamazapine, colchicine, propylthiouracil, methimazole
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What drugs (5) can cause agranulocytosis as a side effect
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Chloramphenicol, benzene, NSAIDs, propylthiouracil, methimazole
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What drugs (5) can cause Aplastic anemia as a side effect
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Methyldopa
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What drug can give a direct positive coomb's hemolytic anemia?
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Chloramphenicol
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What drug can cause grey baby syndrome as a side effect
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INH, sulfonamides, primaquin, aspirin, ibuprofen, nitrofurantoin (hemolysis IS PAIN)
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What drugs (6 - mnemonic) can cause hemolysis in G6PD patients.
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OCPs (estrogen and progestins)
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What drug class can cause thrombotic compications as a side effect?
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ACE inhibitors (NOT ARBs)
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What drug causes a dry cough as a side effect?
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Bleomycin, busulfan, amiodarone
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What drugs (3) can cause pulmonary fibrosis as a side effect?
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Macrolides
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What drug can cause acute cholestatic hepatitis as a side effect?
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Halothane, valproic acid, acetominophen, Amanita phalloides
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What drus (4) can cause focal to massive hepatic necrosis as a side effect?
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INH
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What drug can cause hepatitis as a side effect?
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Clindamycin, ampicillin
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What drugs (2) can cause psuedomembranous colitis as a side effect?
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Glucocorticoid withdrawal
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What drug can cause adrenocortical insufficiency as a side effect
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Spironolactone, digitalis, cimetidine, chronic alcohol use, estrogens, ketoconazole (Some Drugs Create Awesome Knockers)
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What drugs (6) can cause gynecomastia as a side effect? (mnemonic)
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Tamoxifen, clomiphene
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What drugs (2) can cause hot flashes as a side effect?
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Phenytoin
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What drug causes gingival hyperplasia as a side effect?
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Furosemide, thiazides
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What drugs (2) can cause gout as a side effect
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Corticosteroids, heparin
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What drugs (2) can cause osteoporosis as a side effect?
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Sulfonamides, Amiodarone, Tetracycline (SAT for a PHOTO)
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What drugs (3) can cause photosensitivity as a side effect (mnemonic)?
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Hydralazine, INH, procainamide, phenytoin (it's not HIPP to have lupus)
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What drugs (4) can cause an SLE-like syndrome as a side effect?
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Fluoroquinalones
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What drug causes tendonitis, tendon rupture and cartilage damage as a side effect in kids?
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Expired tetracycline
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What drug causes Fanconi's syndrome as a side effect
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Methicillin, NSAIDs
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What drugs (2) cause interstitial nephritis as a side effect?
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Cyclophosphamide, ifosfamide
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What drugs (2) cause hemorrhagic cystitis as a side effect?
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Quinidine, quinine
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What drugs (2) cause cinchonism as a side effect?
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Lithium, demeclocycline
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What drugs (2) cause diabetes insipidus as a side effect
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Bupropion, imipenem/cilastin
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What drugs (2) cause seizures as a side effect?
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Antipsychotics (typical)
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What drugs cause tardive dyskinesia?
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Metronidazole, cephalosporins (some), procarbazine, 1st generation sulfonylureas
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What drugs (4) cause a disulfiram-like reaction as a side effect
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Polymixins
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What drug causes nephrotoxicity and neurotoxicity as side effects?
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Aminoglycosides, loop diuretics, cisplatin
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What drugs (3) cause nephrotoxicity and ototoxicity as a side effect?
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Queen barb takes Phen-phen and Refuses Greasy Card Shakes (quinidine, barbiturates, phenytoin, rifampin, griseofulvin, carbamazapine, st. john's wart)
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Mnemonic for p450 inducers
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Inhibitors Stop Cyber-Kids from Eating Grapefruit (INH, sulfonamides, cimetidine, ketoconazole, erythromycin, grapefruit juice)
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Mnemonic for p450 inhibitors
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Coadminister with mesna
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Method to prevent hymorrhagic cystitis caused by cyclophosphamide or ifosfamide
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Oxalic acid
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What is ethylene glycol converted to in the body
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Acidosis, nephrotoxicity
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What does oxalic acid (metabolic product of ethylene glycol) cause?
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Formaldehyde and formic acid
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What metabolic products (2) is methanol converted to in the body
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Severe acidosis, and retinal damage
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What are the effects of formaldehyde and formic acid (metabolic products of methanol) in the body?
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Acetaldehyde
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What is ethanol broken down by in the body?
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Alcohol dehydrogenase
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What enzyme breaks down ethylene glycol, methanol, and ethanol?
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Fomepizole
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Inhibitor of alcohol DH
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Sulfa drugs (celcoxib, furosemide, thiazides, TMP-SMX, sulfonyureas, sulfasalazine
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What drugs do you not give people with sulfa allergies
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Ephedra
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Herbal agent that can cause arrythmias, stroke, and seizures at high doses
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Feverfew (migraines) and ginko (claudication)
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Herbal agents that have antiplatelet actions
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Kava (chronic anxiety)
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Herbal agent that can cause phototoxicity and dermatotoxicity
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Saw palmetto (benign prostatic hyperplasia)
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Herbal agent that can cause hypertension
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St. John's wort (depression)
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Herbal agent that can cause serotonin syndrome w/ ssris, and induces p-450
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Dehydroepiandosterone (SLE or AIDs)
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Herbal agent that causes androgenization in premenopausal women, and estrogen effects in postmenopausal women and feminization in young men
