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90 Cards in this Set
- Front
- Back
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Michaelis-Menton curve
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Substrate vs velocity
V max is peak velocity on curve Km is [S] at level of 1/2 Vmax Km high = lower affinity |
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Lineweaver-Burk plot, changes due to inhibitors
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Inverse of MIchaelis-Menton curve
y intercept is 1/Vmax; x intercept is 1/-Km; Slope is Km/Vmax Noncompetitive inhibitor - Km is same, Vmax is reduced Competitive inhibitor - Vmax is same Km is higher |
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Enzyme Kinetic changes due to competitive vs noncompetitive inhibitors
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Competitive - Similar to S, binds active site. Vmax same (can be overcome), Km is higher (lower affinity), reduces potency
Noncompetitive - Not like S, binds another site, Reduces Vmax, unchanged Km, reduced efficacy, can't be overcome |
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Vd calculation
Low, Medium, and High |
Vd = amount in body/plasma concentration
Low (4-8L) - Blood; large/charged molecules or plasma protein bound Medium - ECF, small hydrophilic molecules High - All tissues, small lipophilic molecules, esp. if tissue protein bound |
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Half life calculation
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T 1/2 = 0.7 x Vd / CL
Req. 4-5 half lives at constant infusion to reach steady state |
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Clearance calculation
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rate of elimination/plasma drug concentration
Also equals Vd x Ke (elimination constant) |
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Dosage calculations
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Loading dose - Cp x Vd / F (bioavailability)
Maintenance dose - Cp x CL/F Cp is target plasma concentration; in renal disease maintenance dose is lowered and loading dose is unchanged |
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Drugs zero-order elimination
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Constant rate rather than 1st order elimination (fractional)
PEA (Phenytoin, Ethanol, Aspirin) |
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Phase I vs Phase II reactions in drug metabolism
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Phase I - Reduction, oxidation, hydrolysis to get slightly polar metabolites; lost first in aging
Phase II - Conjugation (Glucouronidation, Acetylation, Sulfation) - VERY polar, inactive metabolites for RENAL excretion |
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What drug metabolism type leads to very different effects from drugs
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MOSTLY acetylation (Phase II) difference
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Noncompetitive antagonist vs partial agonist
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BOTH lower efficacy (max effect) but partial agonist binds same site as full agonist with variable potency, and can be overcome
Noncompetitive antagonist cannot be overcome with substrate |
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Therapeutic index calculation
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LD50/ED50
Safer drugs have HIGHER TI values |
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SNS, PNS, Dopamine, Histamine, Vasopressin receptors, mechanism, and location
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SNS
a1 - Gq - vascular smooth muscle, pupil dilator, GI sphincters a2 - Gi - reduced SNS, insulin, lipolysis, more platelet aggregate b1 - Gs - Heart, renin release, lipolysis b2 - Gs - Vasodilation, bronchodilation, reduced uterine tone, relax ciliary muscle (aqueous humor up) PNS M1 - Gq - CNS, enterics M2 - Gi - Heart (HR and contractility down) M3 - Gq - Increased gland secretions, GI activation, bladder contraction, pupillary constriction, ciliary contract Dopamine D1 - Gs - Relax renal smooth muscle D2 - Gi - NT release modulator Histamine H1 - Gq - nasal and bronchial mucus, contract bronchioles, pruritis and pain H2 - Gs - gastric acid secretion Vasopressin V1 - Gq - Vascular smooth muscle contraction V2 - Gs - H20 permeability in CCT and DCT qiss and qiq till you're siq of sqs |
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Receptors for eye
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a1 - pupilary dilation
b2 - ciliary muscle relax - makes aqueous humor M3 - pupilary relax, ciliary muscle contract - accomodation |
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Metyrosine effect
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Blocks tyrosine to dopamine conversion in terminal of axons (reduced catecholamines)
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Reserpine effect
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Blocks dopamine to NE in vesicles in terminal
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Guanethidine, bretylium effect
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Prevent NE release
Opposite of amphetamine |
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Cocaine, TCAs, amphetamine effect
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Block reuptake of catecholamines (amphetamine also potentiates release)
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Bethanechol, Carbachol, Pilocarpine, Methacholine
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Direct cholinomimetic agents, mimic Ach on muscarinic receptors
Activate bowel, bladder, PNS activation Bethanechol - used for GI Carbachol, Pilocarpine - used in eye (glaucoma to reduce pressure) Methacholine - asthma challenge test |
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Neostigmine, Pyridostigmine, Edrophonium, Physostigmine, Donezepil
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Anticholinesterases, indirect cholinergic agonists
Increase Ach effects (myasthenia gravis, alzheimer's etc) Physostigmine and Donepezil cross CNS |
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Cholinesterase inhibitor poisoning
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Massive muscarinic activation; seen in organophosphates
DUMBBELSS Diarrhea Urination Miosis Bronchospasm Bradycardia Excitation of skeletal muscle and CNS Lacrimation Sweating Salivation Antidote is atropine and pralidoxime (regenerate AChE) |
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Atropine, homatropine, tropicamide
Benztropine, Scopalamine, Ipratropium, tiotropium Oxybutynin, Glycopyrrolate |
Muscarinic antagonists, BLOCK effects. Opposite of dumbells
Used to produce mydriasis (atropine), Parkinson's treatment (Benztropine), Motion sickness (Scopalamine), COPD, asthma (Ipratropium; tiotropium), bladder urgency (Oxybutynin), secretions (Glycopyrrolate) |
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Atropine overdose
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Muscarinic antagonist, seen in Jimson weed (gardener's pupil)
High TEMP, dry, flushed skin, cycloplegia, constipation, disorientation Hot as a hare, Dry as a bone, Red as a beet, Blind as a bat, Mad as a hatter Can cause glaucoma (mydriasis), urinary retention |
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Epinephrine vs Norepinephrine effect
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Both SNS agonists
Norepi DOES NOT cover B2 |
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Isoproterenol
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B1 and B2 agonist
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Dopamine
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Low dose is D1 effect (renal perfusion)
medium dose is B1 and B2 agonist high dose is A1 and A2 agnoist |
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Dobutamine
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B1 agonist
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Phenylephrine
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A1 agonist, used for rhinitis (reduce secretions, hypotension, ocular procedures
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Albuterol, Salmeterol, Terbutaline, Ritodrine
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B2 agonists, used for acute asthma or COPD, reduce premature uterine contractions (terbutaline, ritodrine)
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Norepinephrine vs Isoproterenol in HR and BP
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Norepinephrine a1, a2, B1 - raises SBP, DBP. Higher BP causes reflex bradycardia
Isoproterenol - B1, B2 agonist, B2 lowers preload (vasodilation), raises HR, lowers SBP |
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Clonidine, a-methyldopa
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Central a2 agonists, reduce central SNS outflow
Used for HTN in renal disease |
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Pneoxybenzamine, Phentolamine
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alpha blockers (a1 and a2)
Reduce HTN (pheochromocytomas, MAOi pts with tyramine OD) but can cause reflex tachycardia and orthostatic hypotension Phenoxybenzamine is irreversible, Phentolamine is not |
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Prazosin, Terazosin, Doxazosin, Tamsulosin
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A1 selective blockers
Reduce HTN, relax sphincters (BPH urinary retention) |
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Mirtazapine
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A2 blocker, used for depression
Can cause sedation, raise cholesterol |
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Acebutolol, Betaxolol
Esmolol, Atenolol, Metoprolol |
A BEAM
B1 antagonists Used to treat Heart symptoms without any pulmonary side effects (no B2 blockage, so no constriction) |
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Propranolol, TImolol, Nadolol, Pindolol
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Please Try Not Being Picky
Nonselective B blockers, block heart and lung effects, and vascular |
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Carvedilol, Labetalol
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Non selective a and b antagonists
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Antidote: Acetaminophen
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N-acetylcysteine (replenish glutathione)
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Antidote: Salicylates
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Early resp. acidosis, late metabolic acidosis
NaHCO3 to alkalinize urine, dialysis |
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Antidote: Amphetamines
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NH4Cl
Acidify urine |
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Antidote: AChE inhibitors, organophosphates
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Atropine, pralidoxime
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Antidote: Amtimuscarinic, anticholinergicss
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Physostigmine salicylate, control hyperthermia
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Antidote: B blockers
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Glucagon
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Antidote: Digitalis
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Normalize K+, Lidocaine, Anti-dig Fab, Mg2+
KLAM |
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Antidote: Iron
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Deferoxamine, deferasirox
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Antidote: Lead
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CaEDTA, dimercaprol, succimmer, penicillamine
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Antidote: Mercury, arsenic, gold
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Dimercaprol, succimer
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Antidote: Copper
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Penicillamine
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Antidote: Cyanide
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Nitriate + thiosulfate, hydroxocobalamin
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Antidote: Methemoglobin
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Methylene blue, Vit C
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Antidote: CO
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100% oxygen, hyperbaric
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Antidote: Methanol, ethylene glycol
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Fomepizole > ethanol, dialysis
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Antidote: Opiods
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Naloxone, naltrexone
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Antidote: Benzodiazepines
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Flumazenil
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Antidote: TCAs
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alkalinize plasma NaHCO3
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Antidote: Heparin
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protamine
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Antidote: Warfarin
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Vit K, Fresh frozen plasma
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Antidote: tPA, streptokinase, urokinase
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Aminocaproic acid
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Antidote: Theophylline
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B-blocker
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Drug ASE: Cutaneous flushing
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VANC
Vancomycin, Adenosine, Niacin, Ca++ channel blockers |
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Drug ASE: Torsades de pointes
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Class III (sotalol) and class IA (quinidine) antiarrythmics
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Drug ASE: Agranulocytosis
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Agranulocytosis Could Certainly Cause Pretty Major Damage
Clozapine, Carbamazepine, Colchicine, Propylthiouracil, Methimazole, Dapsone |
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Drug ASE: Aplastic anemia
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Chloramphenicol, benzene, NSAIDs, PTU, methimazole
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Drug ASE: Gray baby syndrome
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Chloramphenicol
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Drug ASE: Hemolysis in G6PD def
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hemolysis IS PAIN
Isoniazid, Sulfonamides, Primaquine, Aspirin, Ibuprofen, Nitrofurantoin |
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Drug ASE: Megaloblastic anemia
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Have a blast with PMS
Phenytoin, Methotrexate, Sulfa drugs |
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Drug ASE: Focal to massive hepatic necrosis
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HAVAc
Halothane Amanita phalloides Valproic acid Acetaminophen |
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Drug ASE: Hepatitis
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INH
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Drug ASE: Pseudomembranous colitis
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Clindamycin (lobar pneumonia)
Ampicillin |
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Drug ASE: Gynecomastia
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Some Drugs Create Awkward Knockers
Spironolactone Digitalis Cimetidine chronic Alcohol use estrogens Ketoconazole |
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Drug ASE: Hypothyroidism
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Lithium, amiodarone, sulfonamides
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Drug ASE: Myopathies
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Fish N CHIPS Give you myopathies
Fibrates Niacin Colchicine Hydroxychloroquine IFNa Penicillamine Statins (esp with fibrates) Glucocorticoids |
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Drug ASE: Photosensitivity
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SAT for a photo
Sulfonamides Amiodarone Tetracycline |
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Drug ASE: Rash (Stevens-Johnson syndrome)
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Bad rash after a PEC SLAPP
Penicillin Ethosuximide Carbamazepine Sulfa drugs Lamotrigine Allopurinol Phenytoin Phenobarbital |
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Drug ASE: Drug induced lupus
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not HIPP to have lupus
Hydralazine Isoniazid Procainamide Phenytoin |
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Drug ASE: Tendonitis, tendon rupture, cartilage damage
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Fluoroquinolones (-floxacin) in young children
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Drug ASE: Interstitial nephritis
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Methicillin
NSAIDs Furosemide |
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Drug ASE: SIADH
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Carbamazepine, Cyclophosphamide
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Drug ASE: Cinchonism
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Quinidine, quinine
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Drug ASE: Parkinson-like symptoms
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Antispychotics (halperidol), reserpine, metoclopramide
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Drug ASE: Seizures
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With seizures, I BITE My tongue
Isoniazid Bupropion Imipenem/cilastatin Tramadol Enflurane Metoclopramide |
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Drug ASE: Antimuscarinic
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Atropine
TCAs H1 blockers (diphenydramine) Neuroleptics |
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Drug ASE: Nephrotoxicity/ototoxicity
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Aminoglycosides
Vancomycin Loop diuretics Cisplatin |
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P-450 Inducers
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Momma Barb Steals Phen-phen and Refuses Greasy Carbs Chronically
Modafinil Barbiturates St. John's wort Phenytoin Rifampin Griseofulvin Carbamazepine Chronic alcohol use |
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P-450 Inhibitors
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MAGIC RACKS in GQ
Macrolides Amiodarone Grapefruit juice Isoniazid Cimetidine Ritonavir Acute alcohol Ciprofloxacin Ketoconazole Sulfonamides Gemfibrozil Quinidine |
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Sulfa drugs
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Popular FACTSSS
Probenecid Furosamide Acetazolamide Celecoxib Thiazides Sulfonamide antibotics Sulfasalazine Sulfonylureas Can cause rash, UTI, Stevens johnson, hemolytic anemia, thrombocytopenia, agranulocytosis, urticaria. Very variable |
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Drug ASE: Hyperglycemia
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Niacin
Tacrolimus Protease inhibitors HCTZ Corticosteroids |
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Drug ASE: Gingival hyperplasia
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Phenytoin
Verapamil |
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Drug ASE: Gout
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Furosemide
Thiazides Niacin Cyclosporine |
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Drug ASE: Fanconi's syndrome
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Expired tetracycline
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