Pharmacology Flashcards
(126 cards)
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)