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Drug biotransformation: takes place in almost any tissue in the body, the most important being
the liver. The most important site within the liver cells is the smooth endoplasmic reticulum. This
is a thin tubular network inside the cell that participates in biotransformation. (When the liver is
homogenized, the endoplasmic reticulum is broken up into microsomes).
In a competitive enzymatic reaction, the rate of the reaction is not affected by the addition of
more substrate
(E + S
ES P).
Enzymes (apoproteins): these are protein in nature, used to catalyze biological reactions.
Ligase enzyme: rebuilds DNA which has been destroyed.
Amylase: is a pancreatic enzyme involved in the breakdown of starch. It is elevated in acute
pancreatitis.
Chymopapin: is a proteolytic enzyme used to treat herniated lower back disks.
Pancrease: is most commonly used in patients suffering from:
Cystic fibrosis of pancreas.
Chronic pancreatitis.
Ligases: are one of the 6 main classes of enzymes. These enzymes catalyze the formation of
bonds between 2 substrate molecules coupled with the hydrolysis of pyrophosphate bond in ATP
or similar energy donor.
Protein Kinase: is activated by cyclic AMP (cAMP) & has regulatory subunits; its function is
limited by some enzymes.
The typical cell contains the endoplasmic reticulum, responsible for the degradation of HB.
Cytochrome P 450: is associated with the extra-mitochondrial electron transfer in the liver,
involved in Mixed Function Oxidation reaction in the liver & drug detoxication. It is an ironprotoprophyrin cellular pigment.
Plasma protein binding: If drug B has greater affinity (er association constant) for a specific
protein binding site than drug A. It will displace it. The larger the dose of drug B the greater the
displacement (competitive reaction).
Hemoglobin: is made of 4 protein chain subunits (globulins), each chain containing one haem
moiety. Haem consists of a tetra-pyrrole prophyrin ring containing Fe. Each haem can carry an
oxygen molecule.
(end products)
(end products)
(end
products)
Barbiturates ( & their analogues e.g. glutathemide) induce liver microsomal enzyme system &
increase liver biotransformation.
Phenytoin induces the liver microsomal enzyme system disturbs folic acid metabolism.
Disulfuram & Metronidazole: inhibit the metabolism of alcohol by inhibiting the alcohol
dehydrogenase enzyme. Such drugs should not be given with alcohol because of the possibility
of inducing disulfuram like reactions by inhibiting oxidation of acetaldehyde.
Barbiturates
Phenytoin
Sulfa
Erythromycin
Ethanol
Nicotine
Quinolones
Chloramphenicol
Carbamazepine
Rifampicine
Miconazole
Cimetidine
Allopurinol
A substance that exists naturally in the body is called endogenous / endogenic.
Adjustment of the pH of body fluids: the immediate local adjustment of pH in body fluids is
accomplished by buffers but the eventual disposition of acid (H +) is accomplished by lungs &
kidney (i.e. the regulation of acidosis is 1 st through the blood followed by lungs & kidney).
Adenine
&
Guanine
(purine bases)
Thionine
&
Cytosine
(pyrimidine bases)
Adenine
&
Guanine
(purine bases)
Uracil
&
Cytosine
(pyrimidine bases)
In RNA
Ribose
In DNA
Deoxyribose
N.B.
Essential amino-acids: these are amino-acids that can not be synthesized in the body & must
be taken with diet. They include:
P H I LM VAL T T
Phenyl-alanine Histadine
Isoleucine
Leucine
Methionine
Valine
Arginine
Lysine
Tryptophan
Threonine
Stearic acid: is a saturated fatty acid (18 carbons) with the formula CH 3(CH2)16COOH.
Hemoglobin & cytochrome: are similar in the portion of prophyrin protein (heme protein)
The mitochondria (power house): contains all enzymes responsible for aerobic oxidation.
At a pH below the iso-electric point (IEP), a protein will carry a +ve charge & will migrate
to the ve pole & vice versa. At a pH = IEP, it will ppt & will not migrate to either pole.
1.
2.
3.
4.
5.
6.
a.
b.
Metabolite
b.
Exogenous substance
d.
Hydroxylation
b.
Methylation
c. Acetylation
oxidative deamination
Drugs that induce liver microsomal enzymes & increase its own metabolism are known to be
associated with:
a.
Carcinogenicity
b.
Dependence
c. Tolerance
Ribose
b.
Arabinose
c. Desoxyribose
Proteins.
b.
c. Fats (duodenum)
Proteins.
a.
Carbohydrates.
c. Fats.
a.
c.
c. Substrate
Which is not related to lymphocytes (which is not part of the lymphatic system:
a.
Spleen.
b.
Thoracic duct.
c.
Thyroid
e. Tonsils
1.
Pancreas.
f. Cisterna chyli
Oxidation.
(OH gp)
b.
Reduction.
(NO2 gp)
c.
Glucoronidation. ( N )
d.
Deamination.
NO2
(Only 1ry amines undergo deamination)
OH
N
O
b. Pituitary
c. Adrenal cortex
12. When a pro-drug is converted inside the body to the active form, the phenomenon is called:
a. Bio-activation.
b. Metabolism
c. Bio-transformation.
13. Which of the following agents protect the integrity of the cell (protects the cell from damage):
a. Glutathione
c. Cytochrome oxidase
b. Vitamin E
d. Cytochrome P 450
e.
Methionine
HO
HO
e. An essential amino-acid
CH2CH COOH
NH2
d. Ribose.
b. Uracil.
e. Adenine.
b. Ribose
17. Which may give a false +ve test with 5 hydroxy indole acetic acid (5 HIAA) test:
11. NaCl d. Mephenesine
12. Glyceryl guaiacolate
e. Ampicillin
a. Tetracycline
18. Which of the following enhances the activity of azathioprine (Imuran) by enzymatic oxidation
inhibition:
a. Allopurinol
d. Trimethoprim
e. Scar tissue
c. Teeth
11. Which is the degradation process of desipramine:
a. Demethylation.
b. Alkylation c. Hydrolysis
d. Ketones
b. Gastric juice
c. Blood sugar
22. The main carbohydrate of blood is:
a. D-fructose.
c. D-glucose
b. Mannitol
d. L-glucose
e. Sorbitol.
23. Between particulate & miceller constituents in cells exists an aqueous phase which contains:
a. Soluble protein
e. Electrolytes
25. The presence of mitochondria in the living cell can be detected by:
a. Neutral red.
c. Phenolphthalein.
b. Methylene blue.
e. Janvs green.
c. Cellulose
a. Lactose
d. Erythrose
e. Fructose ????
c. Thymus
a. Pancreas
d. Adrenal cortex
e. Spleen
c. Folic acid
a. Biotin
d. Niacin
e. Thiamine
c. An enzyme acts a:
21. Catalyst
b. Media
c. Cytochrome A
21. Cytochrome G
d. Cytochrome 27
b. Lipids
d. Form a zwitterion
c. Exhibit no migration
34. Colchicine can give a false +ve result for test of:
a. Glucose
d. Ketones
b. Uric acid
e. RBCs
c. Ureates
35. Keratin is a(n):
a. Protein
d. Peptin
b. Albuminoid
e. Ketone
c. Glutetin
36. Oxidation n humans is mediated by:
a. Ozones
d. Glucoronidase
b. Amylases
e. Co-enzyme A
c. Tryptophan
37. Butazol is used for clinical testing of:
32. Thyroid function
d. Liver function
d. 1-2 months
33. 6 14 days
a. 3 weeks
b. The metabolic degradation of Hb takes place in:
32. The reticulo-endothelial system d. Kidney tubules
33. RBCs
d. Formation of biliuredine
b. Formation of urobilinogen
d. Leucine
b. Protine
e. Histadine
c. Glycine
45. An important enzymatic reaction involved in muscular contraction is:
a. Glucose-6-phosphate
b. Glycogenolysis
d. Enolase
d. Coronary occlusion
d. Reduction
42. Acetylation
e. Hydrolysis
a. Glucoronic acid
(glycine or glutamine)
49. Nucleic acids DNA & RNA play an important role in the biosynthesis of protein. The sugar
inherent to their structure is:
a. Glucose
d. Sorbose
b. Sucrose
c. Fructose
50. Some tissues form lactic acid under anaerobic conditions. This phenomenon, specially
characteristic of tumor tissue, is termed:
a. Anerobic glycolysis
( lactic a)
c. B & C.
52. R NH2 + a
-- b -- >
c. Basophiles.
b. Eosinophils.
(secretory function)
b. Mitochondria.
(power house)
c. Cytochrome.
d. Endoplasmic reticulum.
55. Metabolism is enhanced by:
a. Passive reabsorption.
a. What type of reaction is it when there is acetylation of sulphonamides at the amino gp:
49. It is a phase II reaction.
b. What is another name for metabolites present in the body:
a. Endogenic substances.
49. Which of the following is more in plasma than in interstitial fluid:
a. Proteins (Albumin).
b. Na+.
c. K+.
59. A person with blood group AB can receive blood from a person with blood group:
a. AB c. A
e. O
b. A
d. B
60. A woman with hemophelia & her husband has hemophelia which cannot be her daughter:
a. A girl without hemophelia
61. What does each of the following denote:
a. XX
Ban baby.
b. XXXY
c. OX
Turners syndrome
Kleinfilters syndrome
c. Glucoronidation
b. Deamination
d. Hydroxylation
b. Phase II
73. The thin tubular network in the cell that participates in biotransformation is:
a. The smooth endoplasmic reticulum
74. Which does not undergo biodegradation:
a. Poly-L-lactic acid b. Poly-D-lactic acid
75. What is the similarity between Hb & cytochrome P 450:
a. Both contain heme as prosthetic gp (heme portion)
76. Which of the following is a phase I biotransformation:
a. Sulfoxidation
b. Acetylation
b. Thirst
c. Polyuria
b. t-RNA (transfer)
c. r-RNA (replicant)
b. Heating
b. Esterase c. Amidase
b. Histamine
f. Thyroxin
b. Glycine
c. Glutamine
b. Type II hypersensitivity
b. Sulpha
c.
Cimetidine
d. Barbiturates
f. Rifampicine
b. Nicotine
e. Glutathemide
g. Phenytoin
b. Conjugation
c. Beta oxidation
b. DNA replication
b. SrCr
b. Cytochrome G
c. Myotropin
b. Myosin
d. Tropsonin
c. Prolactin e. ACTH
b. GHd. Adrenocortecoids
f. Thyroxin
b. Glycine
c. Glutamine
b. Type II hypersensitivity
b. Sulpha
c.
Cimetidine
d. Barbiturates
f. Rifampicine
b. Nicotine
e. Glutathemide
g. Phenytoin
103.Cholestyramine ???
a.
b. Conjugation
c. Beta oxidation
b. DNA replication
b. SrCr