Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

MN Pharmacology > Pharmacokinetics > Flashcards

Pharmacokinetics Flashcards

1
Q

What are some drugs/properties that are inducers?

A

Anticonvulsants:
Phenobarbitone, Phenytoin, CBZ
Anti-TB: Rifampin
Omeprazole
Griseofulvin
St. John’s work
Cigarette Smoking

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What are some drugs/properties that are inhibitors?

A

Erythromycin,
* Cimetidine
* Grapefruit juice
* Disulfiram
* Ethanol
* Antifungals: Itraconazole,
Ketoconazole
* Antivirals: Ritonavir, Saquinavir

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is consider phase I metabolism?

A

Oxidation, reduction, hydrolysis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What are phase II metabolism?

A

Glucuronide conjugation
Sulfate conjugation
Glutathione conjugation
Acetylation
Methylation
Glycine conjugation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What does drug clearance means?

A

CL= Metabolism + Excretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What condition is caused by a decrease in expression of UGT1A1 glucuronidation?

A

Gilbert syndrome, neonatal hyperbilirubinemia (milder than Crigler Najjar)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

In acetaminophen poisoning, what is the metabolizing mechanism?

A

Metabolized by glucuronidation, Sulfation, oxidation & conjugation with glutathione

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What drugs undergoes acetylation?

A

SUlfonamides, hydralazine, Isoniazid
PAS

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What is Crigler Najjar syndrome

A

Crigler Najjar syndrome is a rare autosomal recessive inherited disorder characterized by the absence or decreased activity of UDP-glucuronosyltransferase, an enzyme required for glucuronidation of unconjugated bilirubin in the liver.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Why are NSAIDs contraindicated in elderly for long term use?

A

NSAIDs inhibit the production of prostaglandins and therefore reduces renal perfusion and GFR.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

**Drugs that are mainly excreted by kidneys

A

Antibiotics such as:
Penicillin, Cephalosporin
Aminoglycosides (gentamycin)
Sulfonamide
Imipinem
Non Steroidal Anti Inflammatory Drugs (NSAIDs) : Aspirin, Paracetamol
Coxibs
Lithium
Digoxin
Immunosuppressant drugs such as Cyclosporine
Anticancer drugs such as Cisplatin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

When would the alkalinization of urine be applicable?

A

When there is salicylates or barbiturate poisoning. (ion trapping to remove weak acids with alkalinization

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What effect does probenecid have on penicillins?

A

It blocks the tubular secretion of penicillin, decrease excretion of penicillin and prolongs penicillin action.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What increases T1/2 in drugs?

A

Impaired renal clearance

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Loading dose is affected by which factors?

A

Target Cp and volume

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What factors is maintenance dose affected by?

A

Clearance rate ,concentration ,half life , and dosing time

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Formula of Half life?

A

Half life= V d / Clearance

18
Q

How many half lives is needed for nearly elimination of a drug?

A

4 to 5 half lives

19
Q

What is constant in first order kinetics?

A

The clearance is constant

20
Q

What is constant in zero order kinetics?

A

The rate of elimination is constant

21
Q

Zero-order kinetics of drug elimination occurs when:

A) The rate of elimination is proportional to the drug concentration
B) The rate of elimination remains constant over time
C) The rate of elimination decreases as drug concentration decreases
D) The rate of elimination increases as drug concentration increases

A

B) The rate of elimination remains constant over time

22
Q

First-order kinetics of drug elimination occurs when:

A) The rate of elimination is proportional to the drug concentration
B) The rate of elimination remains constant over time
C) The rate of elimination decreases as drug concentration decreases
D) The rate of elimination increases as drug concentration increases

A

A) The rate of elimination is proportional to the drug concentration

23
Q

Which variables below contribute directly to the maintenance dose? ( May choose more than 1)

A. Bioavailability
B. Clearance
C. Drug plasma concentration
D dosing interval
E. Volume of distribution

A

A. Bioavailability
B. Clearance
C. Drug plasma concentration
D dosing interval

24
Q

Which variables below contribute directly to the loading dose? ( May choose more than 1)

A. Bioavailability
B. Clearance
C. Drug plasma concentration
D dosing interval
E. Volume of distribution

A

A. Bioavailability
C. Drug plasma concentration
E. Volume of distribution

25
Q

Which of the following drugd do not follow zero order kinetics?

  1. Phenytoin
  2. Ethanol
  3. salicyclates
  4. Paracetamol
A
  1. Paracetamol
26
Q

Role of P glycoprotein

A

Primary Transport drug out of cell- associated with MDR 1 gene.
Role in ADME:
Limit intestinal absorption
Distribution of drugs into brain, testes and fetal tissue, promote biliary and renal elimination

27
Q

Role of SLC transporter

A

Secondary active transport- uses the energy stored in the ion concentration gradient from primary active trasnport (potential energy) to drive the secondary active transport.
It mediates both uptake and efflux of drugs and metabolites.

28
Q

What are the 2 secondary active transport

A

Symport ( Cotransport): both the
solutes move in the same direction
e.g. sodium glucose symporter
Antiport (Counter transport): move in
opposite direction e.g. sodium calcium
exchanger

29
Q

Examples of SLC:

A

OATP-organic anion transporting
polypeptide
* OCTOCT-organic cation transporter
* DAT, NET, SERT : Na+/Cl Cl-dependent
neurotransmitter transporters
* SGLTSGLT1, SGLT SGLT2: glucose transporters in
intestine & renal tubules

30
Q

Drug that undergo substantial first pass elimination

A

Aspirin, GTN, ISDN, Levodopa, Lidocaine, Verapamil, Salbutamol, Morphine, Metoprolol, Propanolol.

31
Q

** Extraction ratio-discuss FPM and BA based on high and low ER

A

Low ER, low FPM, High BA
High ER, High FPM, Low BA

32
Q

What does a large Vd mean

A

Low PP binding, and widely distributed in body fluids

33
Q

Formula of Vd

A

Vd= Dose administered IV/Plasma concentration

34
Q

How does the body metabolize acetaminophen?

A

Metabolized by glucuronidation, sulfation, oxidation & conjugation with glutathione.

35
Q

What happens to first order kinetics at higher dose?

A

Elimination process get saturated, kinetics changes from first order to zero order kinetics

36
Q

Drugs with narrow therapeutic window

A

DIgoxin, aminoglycosides,
anti-arrthmics, lidocaine, warfarin, phenytoins, carbamazepine, valproic acid, theophylline, cyclosporine, tacrolimus, lithium, vancomycin, colistin

37
Q

What is loading dose influenced by?
a. clearance
b. volume
c. T 1/2
d. dosing time

A

b. volume
Loading dose =
target Cp x V.

38
Q

Factors affecting excretion

A

Age, renal clearance, pH of urine, Disease

39
Q

Formula of renal clearance

A

CLr= Excretion rate (CuVu) / Plasma concentration (Cp)

Cu- drug concentration in urine,
Vu= volume of urine in 24hrs

40
Q

Which part of the nephrons is used for excretion mainly?

A

Tubular secretion (main mechanism of excretion)

MN Pharmacology (11 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions