Pharmacology Flashcards
In Michaelis-Menten enzyme kinetics, what is the Km?
Km is the concentration of substrate [S] at 1/2 of the Vmax of the enzyme. Km is inversely related to the affinity of the enzyme for its substrate.
In Michaelis-Menten enzyme kinetics, Vmax is directly proportional to what?
Enzyme concentration
What is a Lineweaver-Burk plot?
Basically the Michaelis-Menten kinetics plot but inversed: x intercept is 1/[S], y intercept is 1/V
What is the formula to calculate T1/2 (half-life)?
(0.693 x Vd) / CL
What is the formula to calculate clearance?
CL = (rate of elimination of drug)/(plasma drug concentration) = Vd x Ke *Ke is elimination constant
What is the formula to calculate Loading dose?
(Cp x Vd) / F
What is the formula to calculate Maintenance dose?
(Cp x CL x tau) / F *tau is the dosage interval
Opioid analgesics lead to what cellular events?
Opening of K channels and closing of Ca channels
What are CYP 450 inducers?
Carbamazepine, phenobarbital, phenytoin, rifampin, griseofulvin
What are CYP 450 inhibitors?
Cimetidine, ciprofloxacin, erythromycin, azole antifungals, grapefruit juice, isoniazid, ritonavir
Which receptors are linked to Gs proteins?
beta1, beta2
Which receptors are linked to Gi/o proteins?
M2, alpha2, CB1, GABAb
Which receptors are linked to Gq proteins?
alpha1, M1, M3
What is zero-order elimination?
Rate of elimination is constant regardless of Cp
What is first-order elimination?
Rate of elimination is directly proportional to the drug concentration. Cp decreases exponentially with time
Overdose with drugs that are weak acids are treated by making the urine more basic or more acidic?
Alkalinize the urine with bicarbonate (trapped in the ionized form)
Overdose with drugs that are weak bases are treated by making the urine more basic or more acidic?
Acidify the urine with ammonium chloride
Are amphetamines weak bases or acids?
Weak bases
Is aspirin a weak base or weak acid?
Weak acid
What is Phase I drug metabolism?
Reduction, oxidation, hydrolysis with cytochrome P450 usually yields slightly polar, water-soluble metabolites (often still active)
What is Phase II drug metabolism?
Conjugation (glucuronidation, acetylation, sulfation) usually yields very polar, inactive metabolites (renally excreted)
What is the antidote to acetaminophen?
N-acetylcysteine (replenishes glutathione)
What is the antidote to AChE inhibitors, organophosphates?
Atropine followed by pralidoxime
What is the antidote to amphetamines?
NH4Cl (acidify urine)
What is the antidote to antimuscarinics, anticholinergic agents?
Physostigmine salicylate, control hyperthermia
What is the antidote to benzodiazepines?
Flumazenil
What is the antidote to beta-blockers?
Glucagon
What is the antidote to carbon monoxide?
100% O2, hyperbaric O2
What is the antidote to copper, arsenic, gold?
Penicillamine
What is the antidote to cyanide?
Nitrite + thiosulfate, hydrocobalamin
What is the antidote to digitalis?
Anti-digitalis Fab fragments
What is the antidote to heparin?
Protamine sulfate
What is the antidote to iron?
Deferoxamine, deferasirox
What is the antidote to lead?
EDTA, dimercaprol, succimer, penicillamine
What is the antidote to mercury, arsenic, gold?
Dimercaprol (BAL), succimer
What is the antidote to methanol, ethylene glycol?
Fomepizole > ethanol, dialysis
What is the antidote to methemoglobin?
Methylene blue, vitC
What is the antidote to opioids?
Naloxone
What is the antidote to salicylates?
NaHCO3 (alkalinize the urine), dialysis
What is the antidote to TCAs?
NaHCO3 (plasma alkalinization)
What is the antidote to tPa, streptokinase, urokinase?
Aminocaproic acid
What is the antidote to warfarin?
Vitamin K, plasma if active bleeding
Which drugs can cause coronary vasospasm?
Cocaine, supatriptan, ergot alkaloids
Which drugs can cause cutaneous flushing?
Vancomycin, adenosine, niacin, CCBs
Which drugs can cause dilated cardiomyopathy?
Doxorubicin and daunorubicin (anthracyclines - chemo)
Which drugs can cause torsades de pointes?
Class III and class IA antiarrhythmics, macrolides, antipsychotics, TCAs
Which drugs can cause adrenocortical insufficiency?
Glucocorticoids
Which drug can cause acute cholestatic hepatitis, jaundice?
Erythromycin
Which drugs can cause focal to massive hepatic necrosis?
Halothane, Amanita phalloides, valproic acid, acetaminophen: “liver HAVAc”
Which drugs can cause pseudomembranous colitis?
Clindamycin, ampicillin, cephalosporins