General

Question 1

What is the half life equation?

Answer 1

T1/2=0.7Vd/CL and t1/2=0.7/Ke

Question 2

What is the loading dose equation? What is the maintenance dose equation?

Answer 2

Loading dose=Cp*Vd/F Maintenance dose=Cp*CL*tau/F

Question 3

Which drugs have 0-order elimination?

Answer 3

Phenytoin, ethanol, aspirin - Cp decreases per time

Question 4

What are examples of weak acid drugs and what is the antidote?

Answer 4

Examples: phenobarbital, MTX, aspirin, TCAs Antidote: bicarbonate

Question 5

What is an example of a weak base drug and what is the antidote?

Answer 5

Amphetamines and the antidote is ammonium chloride

Question 6

Drug efficacy is measured by what?

Answer 6

Vmax

Question 7

How is volume of distribution calculated?

Answer 7

Vd=F*(dose of drug given)/plasma drug concentration

Question 8

How is potency measured?

Answer 8

Lower EC50 correlates with higher potency - less drug needed for same effect

Question 9

How do competitive antagonists change potency and efficacy?

Answer 9

Decreases potency and no change in efficacy

Question 10

How does a noncompetitive antagonist affect potency and efficacy?

Answer 10

Decreases efficacy and cannot be overcome by adding substrate

Question 11

What is the therapeutic index?

Answer 11

Therapeutic index= TD50/ED50= median toxic dose/ median effective dose

Question 12

What kind of receptors are nicotinic and muscarinic receptors and where are they located?

Answer 12

Nicotinic receptors - Ligand ACh gated Na/K channel found at all post synapses from initial neuron. Muscarinic receptors - ACh Gcoupled receptors located in parasympathetic post ganglionic cardiac, smooth muscle, gland cells and nerve terminals and sympathetic post ganglionic sweat glands

Question 13

alpha1 receptors: what is the Gprotein class? What are the major functions it is involved with?

Answer 13

G protein class: Gq; Major functions: Sympathetic NS. Increases vascular smooth muscle contraction (increases BP) , increase pupillary dilator muscle contraction (mydriasis- dilated pupils), increases intestinal and bladder sphincter muscle contraction (prevents peeing and pooping)

Question 14

alpha2 receptors: what is the G protein class? What are the major functions involved?

Answer 14

Gi protein; Functions: Sympathetic NS. decrease sympathetic outflow (negative feedback fxn), decrease insulin release, decrease lipolysis, decrease aqueous humor production, increase platelet aggregation

Question 15

beta1 receptors: G-protein class? Major functions involved?

Answer 15

Gs protein; Functions: Sympathetic NS. increases heart rate and contractility (chronotropic and ionotropic) increases renin release (increases BP), increase lipolysis

Question 16

Beta2 receptors: G-protein class? Major functions involved?

Answer 16

Gs protein; Functions: Sympathetic NS. vasodilation, bronchodilation, increase lipolysis and insulin release (to lesser degree than alpha2 decreasing lipolysis and insulin so there is a net decrease) decrease uterine tone (tocolysis), ciliary muscle relaxation (increases intraocular presssure), increase aqueous humor production

Question 17

M1 receptor: G-protein class? Major functions involved?

Answer 17

Gq protein Functions: Parasympathetic - CNS and enteric nervous system

Question 18

M2 receptor: G-protein class? Major functions involved?

Answer 18

Gi Functions: Parasympathetic NS. decreases HR and contractility of atria (inhibition of atrial nodal area)

Question 19

M3 receptor: G-protein class? Major functions involved?

Answer 19

Gq Functions: Parasympathetic NS. increases exocrine gland secretions (lacrimal, salivary, gastric acid), increase gut peristalsis, increase bladder contraction (pee!), bronchoconstriction, increase pupillary sphincter muscle contraction (miosis), increase ciliary muscle contraction (accomodation)

Question 20

M3 receptor: G-protein class? Major functions involved?

Answer 20

Gq Functions: Parasympathetic NS. increases exocrine gland secretions (lacrimal, salivary, gastric acid), increase gut peristalsis, increase bladder contraction (pee!), bronchoconstriction, increase pupillary sphincter muscle contraction (miosis), increase ciliary muscle contraction (accommodation)

Question 21

D1 receptor: G-protein class? Major functions involved?

Answer 21

Gs Functions: Dopamine receptor. relaxes renal vascular smooth muscle -> allows for increased renal perfusion

Question 22

D2 receptor: G-protein class? Major functions involved?

Answer 22

Gi Functions: Dopamine receptor. Modulates NT release, especially in the brain

Question 23

H1 receptor: G-protein class? Major functions involved?

Answer 23

Gq Function: histamine receptor. “Allergy symptoms” Increases nasal and bronchial mucus production, increases vascular permeability, bronchiole constriction, pruritus, pain

Question 24

H2 receptor: G-protein class? Major functions involved?

Answer 24

Gs Function: histamine receptor. Increases gastric acid secretion from parietal cells

Question 25

V1 receptor: G-protein class? Major functions involved?

Answer 25

Gq Vasopressin (ADH) receptor. Increases vascular smooth muscle contraction (increase BP)

Question 26

V2 receptor: G-protein class? Major functions involved?

Answer 26

Gs Vasopressin (ADH) receptor. Increases water permeability and reabsorption in collecting tubules of kidney ("V**2** is found in the **2** kidneys")

Question 27

What induces cytochrome P-450?

Answer 27

**Chronic alcohol** use **St**. John's wort **Phen**ytoin **Phen**obarbital **Ne**virapine **R**ifampin **Gr**iseofulvin **Carb**amazepine "**Chronic alcoholic**s **St**eal **Phen-Phen** and **Ne**ver **R**efuse **Gr**easy **Carb**s"

Question 28

What are substrates of cytochrome P450?

Answer 28

Anti-epileptics, Theophylline, Warfarin, OCPs

Question 29

What are inhibitors of cytochrome P450?

Answer 29

**A**cute **a**lcohol **a**buse **R**itonavir **A**miodarone **C**imetidine **K**etoconazole **S**ulfonamides Isoniazid (**IN**H) **G**rapefruit juice **Q**uinidine **M**acrolides (EXCEPT Azithromycin) "**AAA RACKS IN GQ M**agazine

Question 30

Which drugs are sulfa drugs? What are symptoms of sulfa allergies?

Answer 30

**P**robenecid **F**urosemide **A**cetazolamide **C**elecoxib **T**hiazides **S**ulfonamide antibiotics **S**ulfasalazine **S**ulfonylureas "**P**opular **FACTSSS**" _sulfa allergy symptoms:_ fever, UTI, Stevens- Johnson syndrome, hemolytic anemia, thrombocytopenia, agranulocytosis, urticaria (hives)