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My Pharmacology > Pharmacokinetics and Pharmacodynamics > Flashcards

Pharmacokinetics and Pharmacodynamics Flashcards

1
Q

Which form of drugs (ionized or non ionized) can cross cells membranes

A

Non-ionized

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2
Q

In order to excrete an acidic drug in the urine in the case of an overdose, which substance can be used as a treatment?

A

Sodium bicarb (NaHCO3)

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3
Q

In order to excrete an basic drug in the urine in the case of an overdose, which substance can be used as a treatment?

A

Ammonium chloride (NH4Cl)

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4
Q

Equation to calculate volume of distribution

A

(Vd)= Dose/Conc

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5
Q

A drug that binds tightly with tissues will have what kind of Vd

A

High Vd

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6
Q

Drugs that exhibit more protein plasma binding are more likely to have drug interactions by what mechanism?

A

Other drugs will try to displace it from the binding protein

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7
Q

Eg. of a drug with a low Vd

A

Warfarin

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8
Q

Eg. of a drug that competes with warfarin for plasma protein binding

What can result from this?

A

Sulphonylureas

Can lead to bleeding toxicity

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9
Q

Eg. of a class of drugs that competes with bilirubin in neonates for plasma protein binding

What can result from this?

A

Sulfonamides

Can lead to kernicterus (brain damage)

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10
Q

A consequence of hypoalbuminemia as it relates to drug levels in plasma.

What can cause hypoalbuminemia?

A

increased free drug level (possible toxcity)

hypoalbuminemia may be caused by (Burns, hepatic & renal disease)

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11
Q

A consequence of hyperalbuminemia as it relates to drug levels in plasma.

What can cause hyperalbuminemia?

A

Decreased free drug level

hyperalbuminemia may be caused by (dehydration)

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12
Q

What kind of drugs are able to cross the BBB

A

Only lipid soluble, non-ionized drugs

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13
Q

What is the mechanism of drug redistribution

A

drugs distribute first to organs with high blood flow then ‘redistribute’ to other tissues such as muscle and fat

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14
Q

Equation for calculating loading dose

A

Loading dose = (Vd) (Css)/F

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15
Q

What is meant by biotransformation

A

Process to increase water solubility, to inactivate the drug, achieved by converting the drug into a more excretable form

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16
Q

What are the 2 phases of biotransformation, where do they occur and what is involved

A

Phase I- Endoplasmic reticulum (Cytochrome P 450)

Phase II- Cytosol (Conjugation)

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17
Q

Inducers of cytochrome P450

A

Carbamazepine, phenobarbitone, phenytoin

Rifampin, chronic alcohol, glucocorticoids, St.John’s wort, Nevirapine, Griseofulvin

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18
Q

Cytochrome P450 requires which two molecules to do its job

A

O2 and NADPH

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19
Q

If a cytochrome P450 inducer is given with a drug, what is expected to be seen and why

A

Reduced efficacy of the drug due to increased metabolism of the drug

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20
Q

If a cytochrome P450 inhibitor is given with a drug, what is expected to be seen and why

A

Increased efficacy of the drug due to decreased metabolism of the drug (could lead to toxicity)

21
Q

Inhibitors of cytochrome P450

A

Cimetidine
Omeprazole
Ketoconazole
Erythromycin

22
Q

Which 3 processes occur during phase !! of biotransformation

A
  1. Glucuronide conjugation
  2. Acetylation
  3. Glutathione (GSH) conjugation
23
Q

an eg. of a type of drug which undergoes glucuronide conjugation

A

oral contraceptives

24
Q

Which drugs, if given to slow acetylators can cause drug induced lupus

A

Sulfonamides
Hydralazine
Isoniazid
Prrocainamide

25
Q

Eg. of a drug which undergoes Glutathione conjugation

A

Acetaminophen

26
Q

Equation to calculate renal clearance

A

Renal excretion rate/ plasma drug concentration

27
Q

Most drugs exhibit which type of kinetics

A

First order kinetics

28
Q

For drugs with first order kinetics the rate of drug elimination is proportional to ________________

A

the plasma drug concentration at any given time

29
Q

Examples of drugs that exhibit zero order kinetics

A

Phenytoin,
Ethanol
Aspirin

30
Q

If drug elimination mechanisms (biotransformation and excretion) become saturated, a drug can exhibit ______-order kinetics

A

zero order

31
Q

For drugs with zero order kinetics, describe the rate of drug elimination

A

the rate of drug elimination is constant.

32
Q

Equation to calculate Half life(t1/2)

A

t1/2 = 0.7/ke (or) 0.7xVd/CL

33
Q

Equation to calculate Clearance (Cl)

A

Cl = ke x Vd

34
Q

Equation to calculate Infusion rate (Ko)

A

Ko = Cl x Css

35
Q

Equation to calculate Loading dose (LD)

A

LD = Vd x Css/F

36
Q

Equation to calculate Maintenance dose (MD)

A

MD = Cl x Css x dosing interval /F

37
Q

What kind of antgonist will reduce the maximal response of the agonist

A

Non-competitive antagonist

38
Q

What kind of antagonist will cause a rightwards shift in the dose-response curve of an agonist

A

Both a competitive antagonist and a noncompetitive antagonist

39
Q

does a left of right shift in the dose-response curve demonstrate an increase in potency

A

Left-shift

40
Q

What are the 3 types of antagonism

A
  1. Pharmacological Antagonism
  2. Physiological antagonism
  3. Chemical antagonism
41
Q

Describe a chemical antagonist

A

Antagonist form a complex with the agonist and reverse its action
No receptors involved

42
Q

Describe a physiological antagonist

A

An agonist response mediated through a receptor is antagonised by an agonist acting on a different receptor

different receptors

43
Q

Describe a pharmacological antagonist

A

An antagonist that uses the same receptor as the agonist

44
Q

What kind of agonist is Buprenorphine, which drug does it interact with

A

A partial agonist. it interacts with morphine

45
Q

How does a ceiling effect occur

A

Addition of the partial agonist on top of a full agonist with 100% response will displace the full against from the receptor

46
Q

What is the therapeutic index

A

The range of doses between the minimal effective concentration and the lethal concentration

47
Q

Diazepam uses which kind of receptor binding

A

Ligand & voltage -gated

48
Q

Which receptors act via Gi signal transduction

A

Muscarinic 2
Alpha 2
Dopaminergc 2

MAD2

49
Q

Which receptors act via Gq signal transduction

A 
Histamine (H1)
Alpha 1
V1
M1,
M3

HAVe 1 MM

My Pharmacology (2 decks)

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