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PHARMACEUTICAL SCIENCES > Metabolism > Flashcards

Metabolism Flashcards

1
Q 
Examples of reactive metabolites:
Meperidine
Morphine
Acetaminophen 
Furosemide 
Sulfamethoxazole 
Cyclophosphamide
A 
Meperidine➡️nor-meperidine
Morphine➡️morphine-6-glucuronide
Acetaminophen➡️benzoquinoneimine
Furosemide➡️furo epoxide
Sulfamethoxazole➡️nitroso sulfomethoxazole
Cyclophosphamide➡️acroleine
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2
Q

Examples of bioactivation (pro-drugs)

A

Cefuroxime auxetil, Methydopa
ACEi Enalapril Ramipril
Valacyclovir➡️vala triphosphate
Fancyclovir➡️pencyclovir

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3
Q

These are biochemical reactions that are catalyzed by enzymes. And examples.

A

yes Phase 1 and 2 metabolism

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4
Q

Phase II metabolism examples

A

Conjugation (ADDITION) metabolism

Glucuronidation, glutathione conjg. sulfonation, acetylation and methylation

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5
Q

Phase 1 metabolism examples

A

Functional grps: OH, NH2, COOH, SH etc
Oxidation reduction hydroxylation deamination dealkylations demethylation oxidative deamination
Cytochrome oxidations (CYP450), reductase, aminase and monoamine oxidase (MAO)

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6
Q

In phase 1, alcohol oxidations yield what?

A 
1* alc oxidation➡️aldehyde➡️acid
2*➡️ketone
3*➡️no oxidation 
methanol➡️formaldehyde ➡️formic acid- causes blindness 
ethanol➡️acetaldehyde
Ethylene glycol➡️oxaldehyde➡️oxalic acid
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7
Q

Both mechanisms are to create a polar substrate to be excreted.
Bacteria resident in the GI tract are involved in this reduction reactions.

A

Oxidation and Reduction.

Azi and Nitro reductions

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8
Q

What drug undegoes Azoreduction?

A

Azoreduction bond (-N=N-)
Sulfasalazine (in gut)➡️ 5aminosalicylic acid (5ASA) + Sulfpyridine
5ASA - Mesalamine

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9
Q

In Nitro reduction, what group does this produces? Drug examples that undergo this nitro and carbonyl reduction.

A

= amine (NH2) group
Chloramphenicol and Clonazepam- Nitro red.
Acetohexamide- carbonyl red.

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10
Q

Two functional groups that undergo hydrolysis, also for fixed oils, give catalyzing enzyme and products.

A

Esters ➡️ by esterases =acid + alcohol
Amide➡️ by amidases= acid + amide
Fixed oils➡️ by ester hydrolysis= glycerol + fatty acids

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11
Q

ASA and Acetaminophen drug metabolisms

A

ASA and SA- glucuronidation, glycine congjn, hydrolysis (major), hydroxylation
Ace- glutathion and sulphate congjn, glucuronidation and phase 1 metabolism

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12
Q

Drug examples that undergo deamination and hydrolysis

A

Deam: Amphetamine and Dopamine
Hydrolysis: Valacyclovir➡️Acyclovir
Famcyclovir➡️Pencyclovir

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13
Q

What metabolism adds glucuronic acid, drugs: aceta, morphine, diazepam, sulfathiazole, digoxin and SA.
What catalyzing enzyme?

A

Glucuronidation by Uridenyl Diphosphate Glucuronyl Transferase (UDP GT)

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14
Q

Ethacrynic acid and acetaminophen (to reduce what toxicity?) undergoes which drug metabolism? By what enzyme?

A

Glutathione conjg by enzyme Glutathione S-transferase (GST)

-reduced hepatotoxicity

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15
Q

1* amines undergo what metabolism (add acetyl grp NH2, OH) by what enzyme and drug examples.

A

Sulfonamides, Isoniazid, Clonazepam and Dapsone

by enzyme N-acetyl transferase

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16
Q

The only amino acid conjugation by what enzyme and drug examples

A

Glycine conj by Acetyl transferase

SA (75% of SA is excreted aft metabolism), Nicotinic acid (Niacin), deoxycholic acid

17
Q

Sulfate conjugation is by what enzyme and what drug examples.

A

Sulfotransferase

Acetaminophen, Methyldopa and Estrone

18
Q

Merhylation is by what enzyme and what drug examples.

A

N-methyltransferase

E, NE, DOPA and Histamine

19
Q

Phase 2 metab. is referred to as what?, parent drug or its metabolite with natural contituents.

A

Conjugation reaction

Glucuronic acid, glutamine, sulfate and glutathione

20
Q

How nutritional status affects drug metabolism.
Low protein diet
Vit. C def
Vit. E def

A

Low protein diet- dec. Oxidative
Vit. C def- Dec. Oxidative pathways
Vit. E def- retards dealkylation and hydroxylation

21
Q

Most common drug metabolizing cytochrome enzyme, also large grp of monooxygenase enzymes resp for toxic hydrocarbons metabolism. Located where?
Give the coenzyme and susbtrate.

A

CYP450 located in ER, also mitochondria membrane and highly concentrated in liver and small intestine
NADPH- coenzyme
O2- substrate

22
Q

Most common enzyme that catalyze phase 1 oxidative reactions.
Most common cytochrome SUBTYPE enzyme is?

A

CYP3A

-CYP3A4

23
Q

This metabolism is for 1* and 2*

A

1*- Steroid and bile acid metabolism

2*- drug metabolism

24
Q

What drugs undergo halogenation?

A

Halothane, Chloramphenicol

25
Q

Species differences between Phase 1 and 2 metabolism

A

1: Quantitative- presence of enzyme inducers and inhibitors
2: Qualitative

26
Q

Physiological or disease states affecting drug metabolism.

A

Liver, renal disease, CHF, hypo hyperthyroidism, alteration of albumin production as in elderly

27
Q

This drug undergoes deamination followed by oxidation and reduction of the ketone formed, N-oxi then N-dealkylation and so on.

A

Amphetamines

28
Q

Oxidation and complete removal of substituents at Carbon 5.
N-dealkylation at N1 and N3
So on

A

Barbiturates

29
Q

In the side chain N10:

N-dealkylation and N-oxidation then scission

A

Phenothiazines

30
Q

Acetylation at N4 amino group
conjg with glucuronic acid:
-or sulfate at N4 amino grp
-or acetylation at N1 amino group

A

Sulfonamides

31
Q

Hepatic microsomal enzymes
Extra hepatic microsomal enzymes
Hepatic non-microsomal enzymes

A

H: Cytochrome IN liver
Extra H: Cyto OUT of the liver
H non: Acetylation, sulfate, GSH, alcohol, dehydrogenase, hydrolysis

31
Q

What enzyme catalyzes most conjugation reactions?

A

UDP GT

32
Q

Most common metabolic reaction in the GI.
Most common phase 1 metabolic reaction.
Most common metabolic reaction in human.

A

Hydrolysis
Oxidation
Glucuronidation

33
Q

Most common CYP3A4 inhibitors?

A

Eryth, Clarith, GFJ, Ketoconazole, Cimetidine, Protease inhibitors

34
Q

Most common CYP3A4 substrates?

A

BZD, statins, Digoxin, Sildenafil

35
Q

Most common CYP2D6 substrate and inhibitor?

A

Codeine and Fluoxetine

36
Q

Most common CYP3A4 inducers.

A

Phenobarbitals, Phenytoin, Carbamazepine, Rifampin, St. John’s Wort

37
Q

Acetaminophen hepatotoxicity can be reduced by?

A

Glutathione conjugation

PHARMACEUTICAL SCIENCES (5 decks)

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