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Pharmacology MBBS > General Pharmacology part 2 > Flashcards

General Pharmacology part 2 Flashcards

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1
Q

Avd of a drug, definition

A

It is the total plasma required to accommodate the administered drug in the whole body at plasma concentration
Avd = (Dose*f)/conc

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2
Q

Loading dose

A

It is the high dose of drug given for drugs with high volume of distribution to maintain a specific plasma concentration
Loading dose = (avd*conc)/f

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3
Q

Factors which affect avd of a drug

A
  1. Lipid solubility
  2. Fat content (hence gender and age)
  3. Plasma protein binding
  4. Specific tissue binding
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4
Q

Digoxin accumulates in which organ

A

Skeletal muscle

Therefore avd is calculated based on lean body mass

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5
Q

Dialysis is not effective in removing toxicity in which cases

A
  1. Increased avd
  2. High plasma protein binding capacity
  3. Which are irreversible binders
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6
Q

Examples of drugs whose toxicity cannot be treated by dialysis

A

O) Opioid and organophosphates

A) Amphetamine
B) Benzodiazepines and beta blockers
C) Ca channel blockers
D) Digoxin

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7
Q

Antidote of benzodiazepines and beta blockers

A

For benzodiazepines it is flumazenil

For beta blockers it is glucagon (source of cAMP)

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8
Q

Antidotes of amphetamines, digoxin and Ca channel blockers

A

Antidote of amphetamine- ammonium chloride

Antidote of digoxin- digiband

For Ca channel blockers it is Ca gluconate

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9
Q

Antidote for opioids and organophosphates

A

Antidote for opioids is naloxone

Antidote for organophosphates is atropine

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10
Q

Free drugs that bind to albumin

A

C. Most CNS drugs like antipsychotics, anti epileptics, benzodiazepines
A. Antibiotics (sulfonamides and penicillin)
N. NSAIDs
W. Warfarin
A. Aspirin
S. Some other examples are also there
Hence warfarin blocks aspirin and vice versa

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11
Q

Drugs that bind to alpha 1 acid glycoprotein

A
  1. Opioids
  2. TCA Tricyclic antidepressants
  3. Anti-arrhythmics (lidocaine, amiodarone, beta blockers)
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12
Q

Conditions in which albumin decreases leading to toxicity of such drugs

A

Nephrotic syndrome
Liver cirrhosis
Chronic kidney disease

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13
Q

Conditions in which there is an increase in alpha 1 acid glycoprotein which leads to decreased efficacy of such drugs

A

Rheumatoid arthritis
Inflammatory bowel disease
Myocardial infarction

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14
Q

Examples of prodrugs

A 
Levodopa
All ACE inhibitors except captopril and lisinopril
Clopidogrel
Famciclovir (antiviral)
Carbimazole (anti thyroid)
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15
Q

Primary purpose of phase 2 of drug metabolism

A

The purpose is to make the drug by conjugation:

  1. Water soluble
  2. Ionised
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16
Q

Functions of phase 1 of drug metabolism

A
  1. Usually drug inactivation
  2. For some drug, it is activation
  3. In the latter part of phase 1 , the water solubility in increased (though by a small amount) by addition of a functional group to the drug
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17
Q

Phase 1 reactions of drug metabolism

A 
O. Oxidation
R. Reduction
C. Cyclisation
H. Hydrolysis
A. Aliphatic or aromatic hydroxylation
D. Deamination
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18
Q

Phase 2 (conjugation) reactions of drug metabolism

A

G. Glucuronation, glycination , glutathionation
A. Acetylation
M. Methylation
S. Sulfation

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19
Q

Most common reactions of phase 1 and phase 2 of drug metabolism

A

For phase 1: oxidation

For phase 2: glucuronidation

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20
Q

Which reactions in drug metabolism are microsomal and which are not

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A

All reactions of phase 1 (mediated by cytochrome p450) and glucuronidation of phase 2 reactions is microsomal
Rest are non-microsomal

21
Q

What does P450 in CYP450 stand for

Study These Flashcards
A

The P stands for pigment and the 450 for the wavelength of light absorbed by the pigment

22
Q

Nomenclature of cytochrome p450. Example CYP1A2

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A

The 1 stands for the family. The A stands for the subfamily.

The 2 stands for the G number

23
Q

Various cytochromes

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A
  1. CYP1A2: TTT
  2. CYP2B6: CM
  3. CYP2C9: PW
  4. CYP2C19: OC
  5. CYP2D6: BOAT
  6. CYP2E1: EE
  7. CYP3A4
24
Q

Drugs which are metabolised by CYP1A2

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A

Tamoxifen
Tacrine
Theophylline

25
Drugs which are metabolised by CYP 2B6
Cyclophosphamide | Methadone
26
Drugs which are metabolised by CYP2C9
Phenytoin | warfarin
27
Drugs which are metabolised by CYP2C19
Omeprazole It activated clopidogrel Note: Omeprazole (used for treating MI) inhibits clopidogrel (used for treating peptic ulcer)
28
Drugs which are metabolised by CYP2D6
Beta blockers antidepressants (TCA, SSRI) antipsychotics opioids-tramadol Activates Tamoxifen
29
Drugs which are metabolised by CYP2E1
Ethanol | Enflurane
30
Drugs which are metabolised by CYP3A4 or | Substrates for P-gp
The most common for drug metabolism Metabolises more than 50% of all drugs Eg., protease inhibitor, statins, amiodarone, cisapride, oestrogen, mifeprestone, erythromycin
31
Atazanavir and irinotecan contradicted in Criggler Najjar syndrome. Why?
These drugs are highly toxic drugs and contradicted in Criggler Najjar syndrome there is a deficiency of glucuronyl transferase
32
Conjugation of drugs | Types
1. Glucuronidation: BAISO 2. Glutathionation: IF 3. Glycination: N 4. Acetylation: SHIPD 5. Methylation: MM 6. Steroids: S
33
Drugs which are conjugated via glucuronidation
``` Benzodiazepines Azatanavir Irinotecan statins oestrogen ```
34
Why is conjugated oestrogen is not excreted
Estrogen glucuronide When it reaches the colon the bacteria secretes glucuronidase which unconjugates the estrogen This causing enterohepatic circulation
35
Antibiotics cause OCP failure. Why?
The antibiotics kill the bacteria which secretes glucuronidase inhibits enterohepatic circulation. The oestrogen levels fall causing OCP failure
36
Drugs metabolised by glutathionation
Ifosfamide | Fosfomycin
37
Drugs metabolised by glycination
Niacin
38
Drugs metabolised by acetylation | What is their side effect
``` Sulphonamides Hydralazine Isoniazid Procainamide Dapsone Side effect is SLE (systemic lupus erthematosus) ```
39
Drugs metabolised by methylation
6-mercaptopurine Methyldopa MM
40
Steroids are conjugated by
Sulfation
41
Drugs which are microsomal enzyme inducers
``` G. Griseofulvin R. Rifampin (imp) A. Alcohol (chronic) B. Benzpyrene P. Phenytoin, phenobarbital, primidone C. Carbamazepine Can cause OCP failure ```
42
Drugs which can cause folic acid deficiency when taken for a long time
Most anti-epileptics like phenytoin, phenobarbital, primidone,carbamazepine cause folic acid deficiency especially when taken for a long time. These are microsomal enzyme inducers
43
Substances other than drugs which cause microsomal enzyme induction
DDT | A plant called St. John’s wort
44
Examples of microsomal enzyme inhibitors are
``` Q. Quinidine I. Isoniazid (sometimes inducer, sometimes inhibitor) C. Cimetidine K. Ketoconazole V. Valproate E. Erythromycin G. Grape fruit juice D. DEC ```
45
Application of microsomal enzyme inhibitors
When ketoconazole (a microsomal enzyme inhibitor) is given with terpenadine (QT elongation), the usually asymptomatic drug causes torsades and death
46
Application of microsomal enzyme inducers
When a young girl on OCP is given rifampicin for tuberculosis, it may cause pregnancy
47
Phases of clinical trials
1. Human pharmacology and toxicity study 2. Therapeutic exploratory trial 3. Therapeutic confirmatory trial 4. Post marketing surveillance (5. Pharmacoepidemiology 0. Microdosing )
48
Adverse effects of drugs
1. Side effects 2. Secondary effects 3. Toxic effects 4. Intolerance 5. Idiosyncrasy 6. Allergy 7. Photosensitivity 8. Dependence and addiction 9. Withdrawal reactions 10. Teratogenicity 11. Mutagenicity and carcinogenicity 12. Drug induced diseases

Pharmacology MBBS (19 decks)

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