Pharmacology

Question 1

In first order kinetics, a drug infused at a constant rate takes about _______ half-lives to reach s-s.

Answer 1

4-5

Question 2

Symbol for bioavailability?

Answer 2

F

Question 3

What are some eg’s of drugs w/zero-order elimination?

Answer 3

PEA (shaped like a zero)
Phenytoin
Ethanol
Aspirin

Question 4

What are the reactions of phase I drug metabolism vs. phase II.

Answer 4

Phase I: reduction, oxidation, hydrolysis via Cyp450 (yield slightly polar, water soluble metabolites)

Phase II: Conjugation (methylation, glucuronidation, acetylation, sulfation- very polar, inactive metabolites)

Question 5

Do elderly pts lose phase I or II of drug metabolism first?

Answer 5

Phase I

Question 6

What defines the therapeutic index? (‘TITE’)

Answer 6

Median toxic dose (TD50) / median effective dose (ED50)

Question 7

Is higher or lower therapeutic index better?

Answer 7

Higher (takes more drug to cause toxicity, and less drug for it to be effective)

Question 8

What to all presynaptic ANS neurons use as their first NT?

Answer 8

ACh- Nicotinic-N (for parasymp & symp)

Question 9

What is the post-synaptic NT that parasymp neurons use?

Answer 9

ACh- muscarinic

Question 10

What are the 3 types of post-synaptic symp NT’s that are released?

Answer 10

NE (a1, a2, B1)
DA (D1)
ACh- muscarinic

Question 11

What tissues receive the muscarinic ACh post-synaptic NT’s in the symp NS?

Answer 11

Sweat glands (only)

Question 12

What tissues receive the dopaminergic post-synaptic NT’s in the symp NS?

Answer 12

Renal vasculature & smooth muscle

Question 13

What tissues receive the NE post-synaptic NT’s in the symp NS?

Answer 13

Everything besides sweat glands, renal vasculature: cardic & smooth muscle, glands, cells, nerve terminals

Question 14

After a pre-synaptic symp nerve interaction w/the adrenal medulla, what 2 NT’s are released?

Answer 14

NE (a1, a2, B1)

Epi (a1, a2, B1, B2)

Question 15

What NT is released in the NMJ for voluntary motor nerves, directly from the sc?

Answer 15

ACh (to nicotinic-M receptors)

Question 16

Actions of symp a1 besides vascular smooth m. contraction?

Answer 16

Increased pupillary dilator m. contraction (mydriasis)

Increased intestinal & bladder sphincter contraction

Question 17

Actions of symp a2 besides decreased symp (adrenergic) outflow?

Answer 17

Decreased insulin release
Decreased lipolysis
Increased platelet aggregation
Decreased aqueous humor production

Question 18

Actions of symp B1 besides increased HR/contractility/renin?

Answer 18

Increased lipolysis

Question 19

Actions of symp B2 besides vasodilation/bronchodilation?

Answer 19

Increased lipolysis
Increased insulin release
Decreased uterine tone (tocolysis)
Ciliary muscle relaxation
Increased aqueous humor production

Question 20

What does symp B3 do?

Answer 20

Increases lipolysis, increased thermogenesis in SkM

Question 21

What are the actions of parasymp muscarinic stimulation?

Answer 21

Decreased HR and contractility of atria
Increased exocrine gland secretions (lacrimal, salivary, sweat, gastric acid)
Increased gut peristalsis
Increased bladder contraction
Bronchoconstriction
Increased pupillary sphincter muscle contraction (miosis)
Ciliary muscle contraction (accommodation)

Question 22

What are the effects of the D1 receptor stimulation?

Answer 22

Relaxes renal vascular smooth muscle

Question 23

What are the effects of the D2 receptor stimulation?

Answer 23

Modulations transmitter release, esp. in brain

Question 24

What are the effects of the H1 receptor stimulation?

Answer 24

Increased nasal and bronchial mucus secretions
Increased vascular permeability
Bronchiolar contraction
Pruritis
Pain

Question 25

What are the effects of the H2 receptor stimulation?

Answer 25

Increased gastric acid secretion

Question 26

What are the effects of V1 (vasopressin) receptor stimulation?

Answer 26

Increased vascular smooth m. contraction

Question 27

What are the effects of V2 (vasopressin) receptor stimulation?

Answer 27

Increased H2O permeability and reabsorption in the collecting tubules of kidney (V2 is found in the 2 kidneys)

Question 28

What is the mnemonic for remembering the G-protein class of symp, parasymp, da, histamine, and vasopressin receptors?

Answer 28

after QISSeS, u get a QIQ out of SIQ SQS SQS = super kinky sex ``` Symp = QISSeS Muscarinic = QIQ Dopamine = SI Histamine = QS Vasopressin = QS ```

Question 29

Fenoldopam: MoA? Uses?

Answer 29

D1 agonist Post-op HTN, hypertensive crisis (beware hypotension/rebound tachyardia)

Question 30

Mododrine MoA?

Answer 30

a1 agonist

Question 31

When do you use penicillamine?

Answer 31

Cu OD

Question 32

1st aid mnemonic for CYP450 inducers? (mnemonic only)

Answer 32

Chronic alcoholics Steal Phen-Phen, Never Refusing Greasy Carbs

Question 33

My mnemonic for CYP450 substrates? (mnemonic + drugs, 4)

Answer 33

The OC's anti-War: Theophylline OCP's Anti-epileptics Warfarin

Question 34

1st aid mnemonic for CYP450 inhibitors? (mnemonic only)

Answer 34

AAA RACKS IN GQ Magazine

Question 35

What are the inducers of "Chronic alcoholics Steal Phen-Phen, Never Refusing Greasy Carbs"?

Answer 35

``` Chronic alcohol St. John's wort Phenytoin Phenobarbitol Nevirapine Rifampin Griseofulvin Carbamezapine ```

Question 36

What are the inhibitors of "AAA RACKS IN GQ Magazine"?

Answer 36

``` Acute alcohol abuse Ritonavir Amiodarone Cimetidine/ciprofloxacin Ketoconazole Sulfanamides INH Grapefruit juice Quinidine Macrolides (except azithromycin) ```

Question 37

What are the sulfa drugs?

Answer 37

"Scary Sulfa Pharm FACTS" ``` Sulfonamide abx Sulfasalazine Probenecid Furosemide Acetazolamide Celecoxib Thiazides Sulfanylureas ```