Basic Pharm

Question 1

The dose-response curve is ….

Answer 1

Determined by receptor bonding characteristics and can determine the ED50

Question 2

Activation of opioid receptor leads to …

Answer 2

Decrease release of neurotransmitters ( increasing K and decreases Ca conductance, neuron becoming hyperporalized and decreases neurotransmitters)

Question 3

Which opioid receptor responsible for respiratory depression?

Answer 3

Mu 2

Mu1: muscle rigidity

Sigma; hallucinations and dysphoria

Question 4

Which the only opioid causes decrease myocardial contractility

Answer 4

Meperidine

Acts like atropine; increases HR, decreases contractility, and mydriasis.

Question 5

Mechanism of Opioid effect on Respiratory depression?

Answer 5

Through blunting CO2 responsiveness (increase apnea thereshold) leading to decrease RR that decreases minute ventilation

The effect are through CNS (decrease central drive to breath).

Question 6

Respiratory depression will return within …. hours after reversal nalaxobe given

Answer 6

2 hours, it’s even sooner with mini-doses 0.4-1 mg

Question 7

Alfentanil vs fentanyl I’m onset?

Answer 7

Alfentanil way faster because it’s the only opioid that is weaker base (pKa 6.8 where the other all above 7.4) resulting in 90% ionized and able to cross BBB rapidly.

Plasma-brain equilibrium t1/2 is 1 minute (fentanyl 6.4 minutes)

Question 8

Sufentanil vs fentanyl?

Answer 8

Both synthetic with very lipid soluble and high protein bound

POTENCY

Fentanyl ~100 times as potent as morphine where sufentanil is just 10 times as potent as fentanyl (way more potent ~1000 compared to morphine)

Question 9

Potency of opioids compared to morphine ?

Answer 9

Sufentanil (1,000) > Remi (300) > fentanyl (100) > Alfentanil (10) > morphine (1) > meperidine (0.1)

The numbers are relative potency compared to morphine

Question 10

What explains that fentanyl has faster onset but it’s t1/2 elimination longer than morphine or all other long acting

Answer 10

Lipid solubility is higher and high volume distribution from central compartments to fat and muscles this terminating it’s effect.

Also it has more protein binding than the other long acting opioids which both delays its elimination

Question 11

Normepridine accumulation in CNS and causes seizures with patients who have coexisted diseases of

Answer 11

Renal failure

Question 12

3 non SSRI meds can cause sweet onion syndrome

Answer 12

Tramadol
Meperidine
Methadone

Question 13

How acetaminophen causes hepatic dysfunction

Answer 13

When acetaminophen is taken in normal doses, it is conjugated in the liver to harmless glu- curonide and sulfate metabolites. These meta- bolic pathways become easily overwhelmed in the setting of a large overdose, however. If this occurs, the cytochrome P450 system directs conversion of the excess acetaminophen to a compound called NAPQI, which is conjugated with glutathione to form a nontoxic mercap- turate metabolite. Once glutathione stores are exhausted in the liver, however, the excess NAPQI combines with proteins within hepatic cells causing hepatic cell death. Taurine is a mercaptan-containing amino acid involved in bile acid biochemistry. Citrulline aids in the detoxification and elimination of ammonia. Ornithine plays an important role in the urea cycle. (Katzung, 2004, p. 36)
N-acetylcysteine should be administered as promptly as possible for treatment of aceta- minophen overdose. It works by helping restore hepatic glutathione stores and by pro- viding sulfhydryl groups that bind toxic metabolites. N-acetylcysteine is administered orally in the form of an initial loading dose (140 mg/kg) followed by 17 doses (70 mg/kg each) given every 4 hours.

Question 14

Dosage equivalent to

(…) Cortisol = hydrocortisone = sole cortisol

(…) Prednisone

(…) Medrals (solumedral)

(…) Dexamethasone

Answer 14

20 C
5 P
4. M
1 D

Question 15

BB selectivity

Answer 15

A-M (B1)

N-Z (B2)

The 2 non selective B and alpha are (carvedilol and labetalol) which they do not have the typical ending suffixes of -olol

Question 16

Medications prolong QT mnemonic

“Some Risky Meds Can Prolong QT”

Answer 16

Satalol
Resperidone
Marcrolides
Chloroquine 
PPI
Quinidine
Thiazides

Question 17

Physostigmine or pyridostigmine that corsses BBB and treat Atropine overdose?

Answer 17

Physo phyxes atropine overdose

The physo phyxes it

PyRIDostiGMine “gets RID of Mysthenia Gracie”

Question 18

G-protein-linked 2nd messenger mnemonic

HAVe 1 M&M3 all cases the Cs

Answer 18

H1 
Alpha 1
V1
M1
And M3 

Work on Gq -> phosphlipase C -> either increase Ca or + protein kinase C -> smooth muscle contraction

All rest other receptors (b1&2, D1, H2, V2, M2, alpha 2, and D2) stimulates either Gs or Gi and dose all the As (Adenylyl cyclase -> ATP to cAMP -> protein kinase A -> increase Ca in heart)

For whether Gs oR Gi remember mnemonic MAD2 (M2, alpha2, D2 -> Gi)

Question 19

Alpha 1 vs 2 function

Answer 19

• Vascular SM contraction
• Mydriasis
• Intestines and bladder sphincter contraction

Alpha 2

• decrease SNS
• decrease insulin release
• decrease lipopysis
• increases plt aggregation

Question 20

Beta 1 vs 2 function

Answer 20

• Tachy and increase conrtactility
• increases renin release
• increases lipolysis

Beta 2

• also Tachy and increase contractility
• lipolysis as well
• vasodilation
• bronchodilator
• increases insulin release
• decrease uterine tone (tocolysis)
• ciliary ms relaxation
• increases aqueous humor production

Question 21

Efficacy vs potency

Answer 21

Efficacy is the maximum effect of a drug. It does not depend on dose.

Potency is the relative dose required to achieve a given effect and is related to receptor affinity.

The potency of a partial agonist may be higher than that of a full agonist. The efficacy of a partial agonist cannot be higher than that of a full agonist.

Question 22

What has the largest volume of distribution? Lipophilic or hydrophilic?

Answer 22

Lipophilic drugs with high affinity for tissue components (tissue proteins, tissue lipids) have a large volume of distribution.

Drugs with high degree of plasma protein binding, low degree of tissue protein binding, and hydrophilic nature have a smaller Vd

Question 23

What is pKa? and what ionized vs nonionized means?

Answer 23

pH which 50% is ionized and 50% is nonionized.

ionized = water soluble 
nonionized = lipid soluble

Question 24

if acidic drug introduced into acidic environment, result will be?

Answer 24

nonionized = lipid soluble and therefore its going to be absorbed.

same if basic drug introduced into basic environment, will produce nonionized and will be absorbed.

it only when basic/acidic drug introduced into opposite environment that will produce ionized form = water soluble and therefore will be peed in urine and wont be absorbed.

Question 25

Elimination is

Answer 25

the change in plasma concentration of a drug divided by the change in time

Question 26

The rate of elimination is constant or linear describes …

Answer 26

Zero order kinetics

A situation where the enzyme or enzymes involved in that particular drug’s metabolism are at maximum capacity or Vmax. In this situation, drug metabolism is independent of drug concentration because the enzymes are saturated.

Question 27

First order kinetics describes a situation where a constant … of a medication is removed per unit time, whereas zero order kinetics describes a situation where a constant … is removed per unit time.

Answer 27

proportion (percentage) -> first order

amount of medication -> Zero order