Pharm (Q/A) Flashcards
Km
Measures the affinity of an enzyme for its substrate ( dec Km = inc affinity)
Vmax
Maximal velocity of an enzymatic reaction (proportional to enzyme concentration)
Competitive inhibition
Does not change Vmax (Lineweaver-Burke lines cross each other “competitively”)
Noncompetitive inhibition
Decreases Vmax (Lineweaver-Burke lines do not cross each other)
Volume of Distribution (Vd)
Drug in body / plasma drug concentration (low Vd (4-8L: in blood), medium Vd (in extracellular space), High Vd (> body weight: in tissues))
Clearance (CL)
Rate of elimination of drug / plasma drug concentration (OR Vd x Kc, where Kc is the elimination constant)
Half life (t1/2)
T1/2 = (0.7 x Vd) / CL
Concentration of a substance after X half lives (1,2,3,4)
1:50%, 2:75%, 3:87.5%, 4:93.75%
Loading dose
= Cp x (Vd / F); (Cp: target plasma conc., F: bioavailability, 1 if by IV)
Maintenance dose
= 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)
Common drugs that follow zero-order elimination
PEA (phenytoin, ethanol, aspirin)
Treating a weak acid overdose
Will get trapped in a basic environment, treat with bicarbonate
Treating a weak base overdose
Will get trapped in an acidic environment, treat with ammonium chloride
Reactions involved in phase I drug metabolism
(Cytochrome P450) 1. reduction, 2. oxidation, 3. hydrolysis (drugs became slightly polarized, may still be active)
Reactions involved in phase II drug metabolism
(Conjugation) 1. acetylation, 2. glucuronidation, 3. sulfonation (drugs become very polarized, are inactivated)
Effect of competitive antagonists on efficacy curves versus noncompetitive antagonists
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)
Effect of partial agonists versus full agnoists on efficacy curves
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)
Therapeutic index (TI)
TILE: TI = LD50 / ED50 (median toxic dose / median effective dose; Safer drugs have HIGHER TI values)
Nm receptors
Receptor location: NMJ; Function: skeletal muscle contraction; Mechanism: ion channel (Na influx)
Nn receptors
Receptor location: Ganglia; Function: stimulates sympathetics and parasympathetics; Mechanism: ion channel (Na influx);
M1 receptors
Receptor location: Nerve endings; Function: Gastric acid secretion; Mechanism: Gq protein;
M2 receptors
Receptor location: Heart; Function: Inhibitory, reduces heart rate; Mechanism: Gi protein;
M3 receptors
Receptor location: Smooth muscle, endothelium, glands; Function: bronchoconstriction, pupil constriction, accommodation, increases secretions; Mechanism: Gq proteins;
alpha1
Receptor location: Arterioles, glands; Function: vasoconstriction (smooth muscle), pupillary dilation, /\ intestine and bladder sphincter contraction; Mechanism: Gq protein;
alpha2
Receptor location: presynaptic nerve endings; Function: inhibitory, feedback inhibition of NT release, \/ insulin; Mechanism: Gi protein;
Beta1
Receptor location: heart, kidney; Function: heart stimulation, renin release; Mechanism: Gs protein;
Beta2
Receptor location: lungs, skeletal muscle; Function: Vasodilation, bronchiole dilation, ciliary process (makes aqueous humour), \/ uterine tone, /\ insulin, /\ lipolysis; Mechanism: Gs protein;
D1
Function: renal vasodilation; Mechanism: Gs protein;
D2
Function: Causes NT release in brain; Mechanism: Gi protein;
H1
Function: /\ mucus production, bronchiole constriction, pain, itching; Mechanism: Gq protein;
H2
Function: gastric acid secretion; Mechanism: Gs protein;
V1
Function: vasoconstriction (smooth muscle); Mechanism: Gq protein;
V2
Function: /\ H20 permeability, reabsorption in collecting tubules in kidney; Mechanism: Gs protein;
$V2 is found in the 2 kidneys$
Mnemonic for gprotein receptors used for D, H, and V receptors
Sick of sex (SIQ, SQS) D1,D2, H1, H2, V1, V2
Function of Gq protein receptors
Gq protein activates PLC, IP3 + DAG, inc Ca++ (IP3) and activate PKC (DAG)
Function of Gi protein receptors
Gi protein activates K+ channels, inhibition of adenylate cyclase, reduction of cAMP
Function of Gs protein receptors
Gs protein activates adenylate cyclase, increases cAMP
Symptoms of cholinesterase inhibitor poisoning (I.e. organophosphates like PARATHION) + Tx
DUMBBELSS (Diarrhea, urination, miosis, bronchospasm, bradycardia, excitation (of skeletal muscle), lacrimation, sweating, salivation); treatment: atropine (reverses symptoms) + pralidoxime (regenerates cholinesterase)
$Ooze from every oriface$
Symptoms of muscarinic antagonist overdose
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
Direct cholinergic agonist drugs
Bethanechol, carbachol, pilocarpine, methacholine
Direct cholinergic agonist; activates bowel and bladder post operation
Bethanechol
Direct cholinergic agonist; used in glaucoma (causes pupillary contraction and reduces ICP)
Carbachol
Direct cholinergic agonist; potent stimulator of sweat and tears
Pilocarpine (PILE on the sweat and tears)
Direct cholinergic agonist; challenge test for asthma diagnosis
Methacholine
Indirect cholinergic agonist drugs (anticholinesterases)
(-stigmine, Ed PHYSted the MAiLman and it ECHOed) Neostigmine, pyridostigmine, physostigmine, edrophonium, echothiophate, malathion
Indirect cholinergic agonist; used in post operative reversal of NMJ block; does NOT penetrate the CNS
Neostigmine (NEO CNS)
Indirect cholinergic agonist; used for myasthenia gravis (due to it’s long action); does NOT penetrate the CNS
Pyridostigmine
Indirect cholinergic agonist; Used for glaucoma and atropine overdose (does cross CNS)
Physostigmine (PHYS is for EYES)
Indirect cholinergic agonist; Used to diagnose myasthenia gravis (extremely short action)
Edrophonium
Indirect cholinergic agonist; used for glaucoma
Echothiophate
Muscarinic antagonist drugs
Atropine, homatropine, tropicamide, benztropine, scopolamine, ipratropium, methscopolamine, oxybutynin, glycopyrrolate, pirenzepine, propantheline
Muscarinic antagonist drug(s); produces mydriasis and cycloplegia (eye)
Atropine (or homatropine, tropicamide)
Muscarinic antagonist drug; treatment for parkinson’s (CNS)
Benztropine (PARK my BENZ)
Muscarinic antagonist drug; treatment of motion sickness (CNS)
Scopolamine
Muscarinic antagonist drug; treats asthma and COPD (respiratory)
Ipratropium
Muscarinic antagonist drug(s); Reduces bladder urgency in cystitis and bladder spasms (GI)
Methscopolamine (or oxybutynin, glycopyrrolate)
Muscarinic antagonist drug(s); treatment of peptic ulcers (GI)
Pirenzepine (or propantheline)
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
Atropine
Nicotinic antagonist; ganglion blocker, used in experimental models to prevent vaga reflex responses to BP changes
Hexamethonium
Low doses of epinephrine are selective for what receptor?
B1
Drug used for anaphylaxis, open angle glaucoma, asthma and hypotension. Binds a1, a2, B1 and B2 receptors.
Epinephrine
Drug used for hypotension. Binds a1, a2 > B1
Norepinephrine
Drug that binds B1 = B2. Used rarely for AV block
Isoproterenol
Drug used for shock (by increased renal perfusion), and heart failure. Binds D1 = D2 > B > a.
Dopamine
Drug used for shock, heart failure, and cardiac stress test. Bind B1 > B2.
Dobutamine
What is the difference in inotropy and chronotropy between dopamine and dobutamine.
Dopamine is inotropic and chronotropic, Dobutamine is inotropic but not chronotropic.
Drug used for pupillary dilation, vasoconstriction, and nasal decongestion. Binds a1 > a2.
Phenylephrine.
Drugs used for acute asthma. Binds B2>B1/
Albuterol
Drug used to reduce premature uterine contractions. Binds B2 > B1.
Terbutaline
Drug used to reduce premature uterine contractions. Binds B2 only.
Ritodrine
Drug used to treat narcolepsy, obesity, ADD. Releases stored catecholamines.
Amphetamine
Drug used for nasal decongestion, urinary incontinence, and hypotension. Releases stored catecholamines.
Ephedrine
Drug that causes vasoconstriction and local anesthesia. Inhibits reuptake of NE.
Cocaine
Drug used to treat hypertension (esp in renal disease because it prevents decrease in blood flow to kidney. Centrally acting a2 agonist.
Clonidine, a-methyldopa
Effect of NE on systolic and diastolic BP, and heart rate.
Increased systolic and diastolic pressure, reflex bradycardia (all because a>B)
Effect of epinephrineon systolic, diastolic BP and heart rate
Increased systolic (B1), decreased diastolic (B2) (wide PP, no change in mean BP), increased heart rate (B1)
Effect of isoproterenol on BP and heart rate
Decrease BP (sys and diastolic, B2), BIG increase in HR (B1) (isoproterenol = B > a)
Mnemonic for selective B2 agonists
MAST (metaproterenol, albuterol, salmeterol, terbutaline)
Drugs (2) used in pheochromocytoma before tumor is removed. SE: orthostatic hypotension, reflex tachycardia
Phenoxybenzamine (irreversible), Phentolamine (reversible, both nonselective alpha blockers)
Alpha antagonist used for hypertension and urinary retention in BPH. SE: first dose orthostatic hypotension
(a1 antagonists) Prazosin, Terazosin, doxazosin
Alpha antagonist used for depression. SE: sedation, inc serum cholesterol, inc appetite.
(a2 selective) Mirtazapine
How do beta blockers effect hypertension
Dec CO, dec renin secretion (B1)
How are B blockers used in MI
Dec mortality after MI
What B blockers are used in supraventricular tachycardia
Propanolol, esmolol
What type of arrhythmia are B blockers used for
Dec. AV conduction velocity (SVT)
How are B blockers used in glaucoma.
Dec secretion of aqueous humor (timolol)
What are the sideeffects of B blockers
Impotence, exacerbates asthma, don’t use with diabetics
What are the nonselective B blockers
Propanolol, timolol, nadolol, pindolol, labetalol
What are the selective B1 blockers (mnemonic)
A BEAM of B1 blockers (acebutolol, betaxolol, esmolol, atenolol, metoprolol)
Nonselective alpha and beta antagonists
Carvedilol, labetalol
Treatment for overdose of acetominophen
N-acetylcysteine
Treatment for overdose of Salicylates
NaHCO3 (alkalinize urine), dialysis
Treatment for overdose of amphetamines
NH4Cl (acidify urine)
Treatment for overdose of anticholinesterases, organophosphates
Atropine, pralidoxime
Treatment for overdose of antimuscainic and anticholinergic agents
Physostigmine saligylate
Treatment for overdose of B blockers
Glucagon
Treatment for overdose of digitalis
K+, lidocaine, digibind, Mg2+
Treatment for overdose of iron
Deferoxamine
Treatment for overdose of lead
CaEDTA, dimercaprol, succimer (kids), penicilamine
Treatment for overdose of arsenic, mercury, gold
Dimercapol, succimer
Treatment for overdose of copper, arsenic, gold
Penicillamine
Treatment for overdose of cyanide
Nitrite, hydroxycobalamin, thiosulfate
Treatment for overdose of methemoglobin
Methylene blue
Treatment for overdose of CO
100% O2, hyperbaric O2
Treatment for overdose of methanol or ethylene glycol (antifreeze)
Ehtanol, dialysis, fomezipol
Treatment for overdose of opiods
Naloxone, naltrexone
Treatment for overdose of benzodiazapines
Flumazenil
Treatment for overdose of TCAs
NaHCO3 (serum alkanization)
Treatment for overdose of heparin
Protamine
Treatment for overdose of warfarin
Vitamin K, fresh frozen plasma
Treatment for overdose of tPA, streptokinase
Aminocaproic acid
Sx: lines on gingivae and long bone epiphyses, encephalopathy and erythrocyte basophilic stippling, abdominal colic, sideroblastic anemia, wrist and foot drop
Lead poisining
Acute poisining = gastric bleeding, chronic poisining = metaboic acidosis, GI obstruction (scarring). MOA = peroxidation of lipids
Iron poisining
What drugs give an atropine like side effect to the cardiovascular system?
Tricyclics
What drugs (2) cause coronary vasospasm as a side effect?
Cocaine, sumatripan
What drugs (4) cause cutaneous flushing as a side effect
Niacin, Ca channel blockers, adenosine, vancomycin
What drugs (2) cause dilated cardiomyopathy as a side effect
Doxorubicin, daunorubicin
What drugs (3) cause torsades de pointes as a side effect
Class III antiarrythmics (sotalol), Class IA (quinidine) antiarrhythmics, cisapride
What drugs (5) can cause agranulocytosis as a side effect
Clozapine, carbamazapine, colchicine, propylthiouracil, methimazole
What drugs (5) can cause Aplastic anemia as a side effect
Chloramphenicol, benzene, NSAIDs, propylthiouracil, methimazole
What drug can give a direct positive coomb’s hemolytic anemia?
Methyldopa
What drug can cause grey baby syndrome as a side effect
Chloramphenicol
What drugs (6 - mnemonic) can cause hemolysis in G6PD patients.
INH, sulfonamides, primaquin, aspirin, ibuprofen, nitrofurantoin (hemolysis IS PAIN)
What drug class can cause thrombotic compications as a side effect?
OCPs (estrogen and progestins)
What drug causes a dry cough as a side effect?
ACE inhibitors (NOT ARBs)
What drugs (3) can cause pulmonary fibrosis as a side effect?
Bleomycin, busulfan, amiodarone
What drug can cause acute cholestatic hepatitis as a side effect?
Macrolides
What drus (4) can cause focal to massive hepatic necrosis as a side effect?
Halothane, valproic acid, acetominophen, Amanita phalloides
What drug can cause hepatitis as a side effect?
INH
What drugs (2) can cause psuedomembranous colitis as a side effect?
Clindamycin, ampicillin
What drug can cause adrenocortical insufficiency as a side effect
Glucocorticoid withdrawal
What drugs (6) can cause gynecomastia as a side effect? (mnemonic)
Spironolactone, digitalis, cimetidine, chronic alcohol use, estrogens, ketoconazole (Some Drugs Create Awesome Knockers)
What drugs (2) can cause hot flashes as a side effect?
Tamoxifen, clomiphene
What drug causes gingival hyperplasia as a side effect?
Phenytoin
What drugs (2) can cause gout as a side effect
Furosemide, thiazides
What drugs (2) can cause osteoporosis as a side effect?
Corticosteroids, heparin
What drugs (3) can cause photosensitivity as a side effect (mnemonic)?
Sulfonamides, Amiodarone, Tetracycline (SAT for a PHOTO)
What drugs (4) can cause an SLE-like syndrome as a side effect?
Hydralazine, INH, procainamide, phenytoin (it’s not HIPP to have lupus)
What drug causes tendonitis, tendon rupture and cartilage damage as a side effect in kids?
Fluoroquinalones
What drug causes Fanconi’s syndrome as a side effect
Expired tetracycline
What drugs (2) cause interstitial nephritis as a side effect?
Methicillin, NSAIDs
What drugs (2) cause hemorrhagic cystitis as a side effect?
Cyclophosphamide, ifosfamide
What drugs (2) cause cinchonism as a side effect?
Quinidine, quinine
What drugs (2) cause diabetes insipidus as a side effect
Lithium, demeclocycline
What drugs (2) cause seizures as a side effect?
Bupropion, imipenem/cilastin
What drugs cause tardive dyskinesia?
Antipsychotics (typical)
What drugs (4) cause a disulfiram-like reaction as a side effect
Metronidazole, cephalosporins (some), procarbazine, 1st generation sulfonylureas
What drug causes nephrotoxicity and neurotoxicity as side effects?
Polymixins
What drugs (3) cause nephrotoxicity and ototoxicity as a side effect?
Aminoglycosides, loop diuretics, cisplatin
Mnemonic for p450 inducers
Queen barb takes Phen-phen and Refuses Greasy Card Shakes (quinidine, barbiturates, phenytoin, rifampin, griseofulvin, carbamazapine, st. john’s wart)
Mnemonic for p450 inhibitors
Inhibitors Stop Cyber-Kids from Eating Grapefruit (INH, sulfonamides, cimetidine, ketoconazole, erythromycin, grapefruit juice)
Method to prevent hymorrhagic cystitis caused by cyclophosphamide or ifosfamide
Coadminister with mesna
What is ethylene glycol converted to in the body
Oxalic acid
What does oxalic acid (metabolic product of ethylene glycol) cause?
Acidosis, nephrotoxicity
What metabolic products (2) is methanol converted to in the body
Formaldehyde and formic acid
What are the effects of formaldehyde and formic acid (metabolic products of methanol) in the body?
Severe acidosis, and retinal damage
What is ethanol broken down by in the body?
Acetaldehyde
What enzyme breaks down ethylene glycol, methanol, and ethanol?
Alcohol dehydrogenase
Inhibitor of alcohol DH
Fomepizole
What drugs do you not give people with sulfa allergies
Sulfa drugs (celcoxib, furosemide, thiazides, TMP-SMX, sulfonyureas, sulfasalazine
Herbal agent that can cause arrythmias, stroke, and seizures at high doses
Ephedra
Herbal agents that have antiplatelet actions
Feverfew (migraines) and ginko (claudication)
Herbal agent that can cause phototoxicity and dermatotoxicity
Kava (chronic anxiety)
Herbal agent that can cause hypertension
Saw palmetto (benign prostatic hyperplasia)
Herbal agent that can cause serotonin syndrome w/ ssris, and induces p-450
St. John’s wort (depression)
Herbal agent that causes androgenization in premenopausal women, and estrogen effects in postmenopausal women and feminization in young men
Dehydroepiandosterone (SLE or AIDs)