PHARMACOLOGY SEM 5 2010/2011

I. Answer the following.

1. Benzodiazepines. (Dr. Manals handouts) Four pharmacological actions : a. Antianxiety b. Hypnosis c. Anticonvulsant effects d. Skeletal muscle relaxation Four clinical uses : a. Anxiety b. Insomnia c. Preanaesthetic medication d. Epilepsy 2. Imipramine (or TCAs). (Dr. Manals handouts) Mechanism of action : Inhibit the neuronal reuptake of NE & 5-HT leading to increased their concentration in the synaptic cleft. Also block -adrenergic, M1 & H1 receptors. Four side effects : a. Postural hypotension b. Sexual dysfunction c. Weight gain d. Sedation 3. Mechanism of action of azelaic acid in acne therapy. (pg. 147) Antimicrobial activity against P. acnes and in vitro inhibitory effect on the conversion of testosterone to dihydrotestosterone. 4. Adverse effects of typical antipsychotic on four different body systems and mechanism of each adverse effects. (Dr. Manals handouts) Type ANS Adverse effects y Loss of accommodation, dry mouth, difficulty urinating, constipation y Orthostatic hypotension, impotence, failure to ejaculate y Parkinsons Mechanism M1 blockade

-adrenoceptor blockade

CNS

Dopamine-receptor

y y

syndrome, akathisia, dystonia Tardive dyskinesia

blockade y y Supersensitivity of dopamine receptors Muscarinic blockade

Endocrine system

Other

Toxic-confusional state Amenorrheagalactorrhea, infertility, impotence Weight gain

Dopamine-receptor blockade resulting in hyperprolactinemia Possibly combined H1 and 5-HT2 blockade

II.

Compare.

a. Itraconazole and fluconazole. (pg. 154-155) Itraconazole Low CSF penetration Drug of choice in dermatophytoses & onchomycosis Less tolerated b. Procaine and lignocaine. (pg. 106) Procaine Ester (-COO-) link between aromatic group and amino terminal few minutes By plasma pseudocholinesterase High Lignocaine Amide (-NHCO-) link between aromatic group and amino terminal few hours By liver Rare Fluconazole High CSF penetration Drug of choice in cryptococcal meningitis Wide therapeutic margin (prophylaxis)

Chemistry

T Metabolism Incidence of allergic reactions III. Problem.

A. A 54-year-old man presents to the emergency room with intense pain in his right eye. Examination reveals a red ring surrounding his iris and an elevated intraocular pressure in the same eye. 1. This episode was triggered by : c. Atropine 2. Drug that causes loss of corneal reflex is : a. Cocaine

3. An active mydriatic is : d. Ephedrine 4. A miotic used in treatment of glaucoma is : a. Pilocarpine 5. List one drug for treatment of each of the following : i. Fungal conjunctivitis Nystatin solution ii. Open-angle glaucoma in a patient having bronchial asthma. Prostaglandin analogue (Latanoprost solution)

B. A 9-year-old child is having learning difficulties at school. He has brief lapses of loss of consciousness with eyelid fluttering that occur every 5-10 minutes. EEG studies reveal brief 3-Hz spike and wave discharges appearing synchronously in all leads. 1. Effective drug in this child is : c. Ethosuximide 2. Adverse effect associated with sodium valproate therapy : d. Hair loss (temporary) 3. False statement concerning proposed mechanisms of action of anticonvulsant drugs : b. Ethosuximide selectively blocks K+ ion channels in thalamic neurons 4. Antiseizure drug that is most likely to elevate the plasma concentration of other drugs administered concomitantly : d. Valproic acid