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ORGMED (LEC) > (P) METABOLIC CHANGES OF DRUGS > Flashcards

(P) METABOLIC CHANGES OF DRUGS Flashcards

1
Q

• Functionalization reactions
• Includes Oxidative, reductive and hydrolytic biotransformations
• Purpose is to introduce a functional polar group(s) (Ex: OH, COOH, NH2, SH) into the xenobiotic molecule to produce a more-water soluble compound

A

Phase 1

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2
Q

• Mixed Function Oxidase System

A

Oxidation

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3
Q

• Responsible for transferring an oxygen atom to the substrate
• Contains Iron and Copper

A

Cytochrome P450 (Wavelength)

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4
Q

Examples of CYP450

A

• CYP3A4
• CYP2D6

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5
Q

most dominant isoform of Cytochrome P450 in the liver

A

CYP3A4

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6
Q

Antidepressants

A

CYP2D6

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7
Q

Cytochrome P450 Enzymes Nomenclature

A

• CYP
• Arabic Number
• Capital Letter

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8
Q

Cytochrome P450 enzymes

A

CYP

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9
Q

• Family (CYP1, CYP2)
• Must have more than 40% identical amino acid sequence
• Individual enzyme in a subfamily (CYP1A2, CYP2C9)

A

Arabic Number

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10
Q

• Subfamily (CYP1A, CYP2C, CYP3A)
• Must have more than 55% identical amino acid sequence.

A

Capital Letter

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11
Q

The CYP enzymes are ____

A

Heme proteins

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12
Q

The heme portion is an iron-containing porphyrin
called ______

A

Protoporphyrin IX

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13
Q

And the protein portion is called ______

A

Apoprotein

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14
Q

• Oxidation of Alcohols

A

Primary: Aldehyde > Carboxylic Acid
Secondary: Ketone
Tertiary: do not oxidize under normal conditions

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15
Q

• plays an important role in the metabolism of many compounds containing carbonyl, nitro and azo group
• carbonyl compounds are converted to alcohol derivatives while nitro and azo are converted to amino derivatives
• Reduction of Aldehydes and Ketones to Alcohol
(Chloral Hydrate (date rape/knock-out drops)&raquo_space; Trichloroethanol

A

Reduction

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16
Q

• for drugs containing the ester/amide functionality
• water is used to breakdown chemical bonds (addition of water)

A

Hydrolysis

17
Q

• Conjugation Reactions
• involve attaching small, polar, and ionizable molecules (like glucuronic acid, sulfate, or glycine) to Phase I metabolites or drugs. This makes them water-soluble, allowing easier excretion from the body through urine or bile.

18
Q

are readily excreted in the urine and are generally devoid of pharmacological activity and toxicity in humans.

A

Conjugated metabolites

19
Q

terminate or attenuate biological activity

A

Methylation and Acetylation

20
Q

protects the body against chemically reactive compounds and metabolites.

A

Glutathione (GSH) Conjugation

21
Q

• Most common
• Morphine, Paracetamol, Chloramphenicol (Gray Baby Syndrome)
• Glucuronyl transferase

A

Glucuronidation

22
Q

• Well-developed in infants
• Ex: Paracetamol

A

Sulfate Conjugation

23
Q

• used to conjugate carboxylic acids
• Ex: Benzoic acid to hippuric acid

A

Glycine & Glutamine Conjugation

24
Q

• an important pathway by which chemically reactive electrophilic compounds are detoxified
• free radical scavenger

A

Glutathione or Mercapturic Acid Conjugation

25
Q

• a tripeptide (glutamyl-cysteinylglycine)

A

Glutathione or GSH

26
Q

• acetyl group utilized is supplied by acetyl CoA
• important for drugs containing primary amino groups
• Hydralazine (SLE), Isoniazid (Peripheral Neuropathy), Sulfonamides (crystalluria)
• uses N-acetyltransferase enzyme
• primary function is to terminate pharmacological
activity and detoxification

A

Acetylation

27
Q

• Systemic Lupus Erythematosus
• autoimmune disease; more common in female
• antigen and antibody complex

28
Q

SLE-like symptom

A

Malar Rash or Butterfly Rash

29
Q

PIMPCH stands for?

A

• Procainamide
• Isoniazid,
• Methyldopa
• Chlorpromazine
• Hydralazine

30
Q

• inactivation of physiologically active biogenic amines
• does not lead to polar or water-soluble metabolites but are pharmacologically inactive

A

Methylation

31
Q

Sites of Drug Biotransformation

A

• Liver
• Intestinal Mucosa
• First-pass effect

32
Q

the most important organ in drug metabolism and
detoxification of endogenous and exogenous compounds.

33
Q

• important site especially for orally administered drug
• contains CYP3A4 isozyme and P-glycoprotein that can capture drug and secrete it back into the intestinal tract.

A

Intestinal Mucosa

34
Q

• orally administered drugs pass through the liver and are susceptible to hepatic metabolism before reaching the bloodstream
• can decrease oral bioavailability

A

First-Pass Effect

35
Q

Drugs Metabolized Extensively by First-Pass Effect

A

• Isoproterenol
• Pentazocine
• Lidocaine
• Propoxyphene
• Meperidine
• Propanolol
• Morphine
• Salicylamide
• Nitroglycerin

36
Q

Enzyme Induction(PPRCC)

A

• Phenytoin
• Phenobarbital
• Rifampicin
• Chronic Alcoholism
• Carbamazepine

37
Q

Enzyme Inhibitors (MEDICKAV)

A

• Metronidazole
• Erythromycin
• Disulfiram
• Isoniazid
• Cimetidine
• Ketoconazole
• Acute Alcoholism
• Valproic Acid

ORGMED (LEC) (6 decks)

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