Examples of active drug changed by biotransformation into another active

Metabolite codeine and morphine

Examples of inactive (prodrugs) changed by biotransformation into active

Drugs enalapril and enalarilat

It is a constant plasma concentration that should be reached and maintained, to obtain the desired
effect of a drug steady state concentration

large dose that is given at the onset of therapy to reach the Css rapidly, useful in acute conditions like
acute heart failure and it is used with drugs of long t1/2 loading dose

is the fraction (%) of the dose given that reaches the systemic circulation bioavailability

It is the time taken by the drug to reach 50% of its original plasma concentration plasma half life

what is the Clinical significance of Vd?

Drugs with high volume of disturbing as digoxin are more distribution in the to tissue large than
plasma and hemodialysis not benefit in drugs toxicity, the aspirin mainly in plasma than tissue so
hemodialysis is effective in treating of drug toxicity

What is the clinical importance of drug clearance?

To calculate the Maintenance dose

As in renal failure select the drugs not depends on the Kindy for clearance

In hepatic failure select the drugs not depends on the liver clearance

What is the Therapeutic importance of t1/2

Mention 2 Indications of TDM

1- Drugs with low therapeutic index ( narrow safety margin) 2- failure of

therapeutic response at usual effect doses 3- renal or hepatic failure to

adjust the drugs dose 4- Diagnosis of drug toxicity

Give 2 examples of desirable drug interactions

Enhanced sedation provide by sedative and opioids 2- combination between aminoglycosides and
penicillin increase the anti bacteria action

Give an example of pharmaceutical drug interactions

Barbiturates mixed with opioids in same syringe make precipitate form

Give an example of pharmacodynamic drug interactions

Naloxone competes with morphine on same receptors so use it for morphine toxicity

Give an example of drug interaction affecting drug absorption

1- Change pH administration of NaHco3 decrease the absorption of aspirin 2- formation of
complex Ca ++ ions present in milk form complex with tetracycline decrease the absorption

Give an example of drug interaction affecting drug distribution

Aspirin and sulfonamides cause displacement of warfarin from plasma proteins binding sites so
increase the warfarin free so cause bleeding

Give an example of drug interaction affecting drug metabolism

The liver microsomal enzymes mainly effect the metabolism of the drugs decrease from effect of
drug so increase the dose Know as HME inducers as phenytoin and phenobarbital and
testosterone

HME inhibitor as cimetidine , contraceptive pill, ketoconazole , erythromycin decrease the

metabolism of drug and increase the effect of drug and drugs toxicity

Give 2 examples of drug interactions affecting drug excretion

Probenecid with penicillin competes on same transport mechanism so decrease the penicillin
excretion

Mention 2 drugs can cause fetal malformations especially if given in early

Aspirin and cortisone, benzodiazepines

pregnancy an example of drug excreted by the lung is inhalation anesthesia

Drug metabolism is affected by genetic polymorphism acetylation of isoniazid is a drug example.

Mention the Mechanisms of absorption of drugs from the GI tract

By passive transport and facilities diffusion, active transport and pinocytosis

What is the role of P-glycoprotein in drug absorption?

Is an efflux transport it pump certain drugs out of the cell

Drug Absorption is affected by Factors related to the drug mention them with drug examples.

1- Lipids solubility aspirin ( weak acid) and Less ionized so increase absorption by gastric mucosa,
amphetamine( weak base) less ionized so well absorption by intestine so must be Less polar
and Less ionized
2- Chemical stability some drugs unstable in acid pH stomach as penicillin , destroyed by digestive
enzymes as insulin

Drug Absorption is affected by many Factors related to the patient, mention 2 of them with drug
examples.

-1- rout of administration in oral administration the drugs absorption is affected by first pass
metabolism

2- GIT motility so increase the motility decrease the content time decrease the absorption
Absorption of vitamin B12 across the gut wall is through which following?

a) passive diffusion b) facilitated diffusion c) active transport d) pinocytosis

Which drug of the following is well absorbed from gastric mucosa?

a) aspirin b) amphetamine c) penicillin G d) insulin

b) Which one of the following is well absorbed from the

intestine?

a) aspirin b) amphetamine c) penicillin G d) insulin

Which one of the following is unstable in the acidic pH of the stomach?

a) aspirin b) warfarin c) penicillin G d) insulin

Which one of the following is destroyed by digestive enzymes?

a) aspirin b) amphetamine c) penicillin G d) insulin

which drug of the following is extensively metabolized by the hepatic first-pass

effect?

a) isoprenaline b) penicillin G c) lidocaine d) warfarin

Which drug of the following shows selective accumulation in bones and teeth?

a) aspirin b) thiopental c) lidocaine d) tetracycline

which one of the following is not correct concerning the drug bound to plasma proteins?

a) it is inactive b) confined to plasma

c) liable to metabolism and excretion d) plasma protein binding is reversible

which drug of the following is highly bound to plasma proteins with high affinity and displaces other
drugs with lower affinity?

a) insulin b) aspirin c) penicillin G d) tetracycline

which drug of the following is highly bound to plasma proteins with high affinity and displace other
drugs with lower affinity?

a) insulin b) sulphonamides c) penicillin G d) tetracycline

b) which one of the following is an example of drug

redistribution?

a) lidocaine b) thiopental c) insulin d) ACE inhibitors according to the FDA

which category of drugs is contraindicated in pregnancy?

a) category A b) category B c) category C d) category X

which one of the following is the main site for drug biotransformation?

a) skin b) kidney c) liver d) lung

Which one of the following is liver microsomal enzyme inducer?

a) contraceptive pills b) ketoconazole c) phenobarbitone d) erythromycin

Which one of the following is a drug that acts through blocking an ion channel?

a) sulfonamide b) aspirin c) lidocaine d) aluminium chloride

Which one of the following is a drug that acts through physical mechanisms?

a) sulfonamide b) aspirin c) lidocaine d) aluminium chloride

Which one of the following is a drug that acts by inhibiting a normal metabolic pathway?

a) sulfonamide b) aspirin c) lidocaine d) aluminium chloride

Glucocorticoid receptor is an example of

a) G- protein coupled receptor

b) Enzyme-linked receptors

c) Intracellular receptors

d) Ligand-gated ion channel receptors

GABAA receptors receptor is an example of

a) G- protein coupled receptor

b) Enzyme-linked receptors

c) Intracellular receptors

d) Ligand-gated ion channel receptors

The antagonism between protamine sulfate and heparin is an example of

a) physical antagonism

b) chemical

c) physiological
d) pharmacological

The antagonism between naloxone and morphine is an example of

a) physical antagonism

b) chemical

c) physiological

d) pharmacological

Which of the following occurs to the antibacterial effect of sulphonamides when trimethoprim is
added?

a) antagonism b) synergism c) addition d) potentiation

Prolonged apnea with succinylcholine in patients with pseudocholinesterase deficiency is an

example of which of the following?

a) hypersensitivity b) cross-tolerance c) idiosyncrasy d) tachyphylaxis

Write an equation to calculate the infant dose.

Write an equation to calculate the child's dose

Give an example of a drug acting through the physical mechanism of action aluminum

chloride a drug that binds to receptors, but gives a partial agonist response is partial

agonist
Prolonged contact of receptors with an antagonist results in up regulations of receptors and
increase drug response

Tendency of a drug to bind to a receptor

a) affinity b) intrinsic activity c) potency d) therapeutic index

Ratio between median toxic dose (TD) and median effective dose (ED) in 50% of the population

a) affinity b) intrinsic activity c) potency d) therapeutic index

decreased response to the drug on repeated administration

a) affinity b) potency c) tolerance d) slope

Tolerance that develops rapidly after the first dose or the first few doses

cross tolerance tachyphylaxis idiosyncrasy hypersensitivity

Development of tolerance to pharmacologically related drugs.

cross tolerance tachyphylaxis idiosyncrasy hypersensitivity

autonomic

Which of the following cholinergic receptors are present in the exocrine glands?

a) M1, M2 b) M1, M3 c) M2 M3 d) M1, Nm

Which one of the following is a directly acting cholinomimetic drug?

a) neostigmine b) organophosphorus compounds c) atropine d) pilocarpine

Mention the mechanism of action and 2 uses of pilocarpine

Direct acting mucrinic agonist

Uses in 1- treatment of glaucoma 2- increase salivary secretion to treat xerostomia

Mention 2 uses and 2 side effects of bethanechol

GIT abdominal cramps and diarrhea 2- urinary bladder frequently to urinate 3- visual disturbances
blurred vision

Mention 2 drugs can be used to treat xerostomia

Cevimeline and Bethanechol and pilocarpine

Which one of the following is used to treat xerostomia?

a) pilocarpine b) ipratropium c) lidocaine d) glycopyrrolate

One of the following is an indication of muscarinic agonists:

a)bronchial asthma c) acute heart failure

b)Patients with complete loss of salivary function d) paralytic ileus

Which one of the following is life-saving in organophosphorus poisoning?

a) pilocarpine b) atropine c) glycopyrrolate d) neostigmine

Mention 3 uses of anticholinergic drugs in dentistry with drug examples whenever possible.

Atropine decrease the flow of saliva during procedure during surgery

Glycopyrrolate has fewer effect on than atropine, More selective anti sialagogue

Mention 3 drugs that can cause xerostomia

Atropine and glycopyrrolate

Mention the mechanism of action and 2 side effects OF atropine

1- Dryness of mouth 2-hot dry skin and increase body temperature 3- blurred vision 4- urine
retention and constipation

Which one of the following is a contraindication to atropine use?

a) bronchial asthma b) benign prostatic hyperplasia c) abdominal colic d) parkinsonism

One of the following is used to decrease the flow of saliva during oral surgery?

a) pilocarpine b) glycopyrrolate c) thiopental d) tropicamide