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UNIT 5 GI > P3 PHARMACOLOGY > Flashcards

P3 PHARMACOLOGY Flashcards

1
Q

any foreign compounds we refer to them as

A

xenobiotics

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2
Q

xenobiotics are normally polar or non polar

A

non polar , lipophilic

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3
Q

in order for xenobiotics to get excreted from body they need to be

A

polar , hydrophilic

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4
Q

most common site for drug biotransformation

A

liver

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5
Q

other sites fro drug biotransformation

A

kidney , lung , brain , intestines

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6
Q

most common type of drug biotransformation

A

from active drug to inactive metabolite

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7
Q

other 3 types of drug biotransformation

A

inactive to active
active drug to active metabolite
Active drug to toxic metabolite

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8
Q

Example of transforming inactive drug to active drug

A

Prednisone to prednisolone

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9
Q

phase 1 of biotransformation includes processes such as

A

Oxidation
Reduction
hydrolysis

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10
Q

the drug after phase 1 will be

A

Slightly hydrophilic

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11
Q

phase 2 processes

A

Methylation
glucuronidation
sulfation , acetylation
glutathione conjugation
amino acids conjugation

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12
Q

why not all drugs get biotransformed

A

Depends on the hydrophilicity

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13
Q

organ eliminating lipophilic drugs

A

liver

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14
Q

organ eliminating hydrophilic drugs

A

kidney

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15
Q

most of phase 1 reactions are achieved by this enzyme

A

Cytochrome P450

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16
Q

the CYTO part comes from

A

the enzyme attachment to ER membrane

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17
Q

the CHROME & P part comes from

A

the enzyme containing heme pigment

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18
Q

the 450 represents

A

the peak activity detected

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19
Q

the CYP represents

A

the superfamily

20
Q

Number 3 represents

A

the family

21
Q

how many cytochrome families are there

A

18

22
Q

the letter A represents

A

the subfamily

23
Q

how many subfamilies are there

A

41

24
Q

the number 4 represents

A

the isoenzyme

25
Q

how many isoenzymes are there

A

around 57 - 60

26
Q

more than 50% of drugs in phase 1 are metabolised by what enzyme

A

CYP3A4/5

27
Q

most of the drugs in phase 2 are metabolised by

A

UDP-glucuronosyltranfase

28
Q

most important factors affecting drug metabolising enzymes

A

Polymorphisms
liver diseases
Drug to drug interactions

29
Q

the genetic polymorphism can result in either …… or …..

A

slow metabolism
or ultra rapid metabolism

30
Q

Increased risk of adverse effects happen due to

A

drug binding to cytochrome enzyme ,
the drug will not undergo metabolism

31
Q

how many doses are needed in drugs that increase the expression of CYP450

A

Several doses

32
Q

Mention some drugs that induce enzyme expression

A

rifampicin and isoniazid

33
Q

mention some drugs that inhibit the enzyme expression

A

sulphamethoxazole , cimetidine , clarithromycin , erythromycin

34
Q

nelfinavir or amprenavir are administered with ritonavir to

A

enhance their activity and reduce the risk of resistance

35
Q

Phenobarbital is used to treat

A

Neonatal kernicterus

36
Q

Phenobarbital induces formation of conjugated bilirubin by inducing

A

UDP gulcuronyl transferase

37
Q

Mention at least 4 factors altering drug effect in liver disorders

A

1-portal systemic shunting 2- alterations in plasma protein binding
3- alterations in liver blood flow 4- alterations in intestinal absorption
5- alterations in hepatic enzymatic activity
6- alterations in biliary excretion 7- alterations in renal excretion

38
Q

why is lidocaine and hydrocortisone administered parenterally

A

to avoid first bypass effect

39
Q

give an example of a drug give via nasal route

A

Desmopressin

40
Q

give an example of a drug given as pulmonary delivery

A

insulin

41
Q

drug given as buccal / sublingual / gingival

A

ISDN

42
Q

drug given as suppository / rectal delivery

A

Diazepam

43
Q

Examples of drugs given vaginally

A

Contraceptives / intravaginal ring

44
Q

drugs that can cause hepatocellular injury

A

Isoniazid & amiodarone

45
Q

drugs that can cause cholestatic injury

A

rifampicin & erythromycin

UNIT 5 GI (34 decks)

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