Semmelweis Pharmacology Semifinal
questions and answers
Local Anesthetics - Correct Answers -Local anesthetics are weak bases, which need a
basic environment to diffuse into the cell, and act on inactivated Na channels
Esters, which are metabolized by esterases (individuals can be fast or slow
metabolizers)
1. cocaine or prococaine - also a NE reuptake blocker, stimuating Alpha 1 receptors
Amines, which are metabolized by liver produced amidases
2. lidocaine
3. articaine the only lipid soluble, so it can move through the membrane.
4. bupivacaine
The effectivness of the Local anesthetic is dependent on the nerve fibres it acts on,
B and c> A(gamma), A(beta) and A(delta)> A(alpha)
Side effects: neurotoxic, cadiotoxic, allergies (PABA)
Alpha 1 agonists are administered with to prevent the spread of the anesthetic
Histamines and Antihistamines - Correct Answers -Autocoid released by Mastcells,
Basophils and platelets. causing T1 Hypersentitivity (anyphylaxis)
H1R>>Gq>>increasing nasal/bronchial mucous secretion,
increase NOS release,
capillary permeability
Bronchial SM contraction
Suppresses AV node
H2R>>Gs>>PKA>>increased Gastric acid secreation
stimulates B1 response, increased HR and contraction
Antagonist
1st Generation: are Lipophylic, allowing them to cross the BBB, thus can be used for
allergic reaction and motion sickness, and nausea and vomiting because they also
block muscurinic receptors. Also induce appetite increase (5HT blocker). Also
antagonize alpha 1R thus induce hypo tension. (cognitive impairment in elderly)
,5. promethazine (alpha blockae and local anesthetic action)
6. diphenhydramine (OTC drug, most effective M blocker and sedator)
9. dimetinden
2nd Generation: are less lypophylic, cannot cross the BB, so only used for allergic
rhinitis with minimal side effects.
7. (levo)cetirizine
8. (des)loratadine
10. fexofenadine
Systemic glucocorticoids (for Oral and Parenteral use) - Correct Answers -
Glucocorticoids are anti-inflammatives and immunosuppressives.
11. hydrocortizone -cortisol supplied as medication, short duration with gluco and
mineralcorticoid action
12. prednisolone - medium duration
13. methylprednisolone- antiinflam
15. triamcinolone - intermediate duration
14. dexamethasone -long duration (most potent) can be used in suppression tests, be
observing ACTH production if its via pituitary or ectopic production (fail)
Mechanism:
-inhibit PLA2, so no Prostaglandins or leukotrienes
no COX2, PAF, IL2
-they decrease the expression of integrins and decrease capillary permeability, thus
decreasing leukocyte migration
-increase lysosomal membrane stability, thus decreasing phagocytosis
Side effects: can induce iatrogenic cushings syndrome by giving cortisol
-suppression of ACTH causes adrenal hypoplasia, so once the treatment stops there is
no endogenous cortisol left, resulting in shock, so the dose must be slowly decreased.
- hyperglycermia due to gluconeogenesis
-Gastric ulcers due to lack of PGE
- electrolyte imbalance due to increased aldosterone (mineralcorticoid action)
-decreased wound healing, increased infection (thrush, candida)
mineralocorticoid, local glucocorticoid, synthesis inhibitor - Correct Answers -16.
fludrocortizone
17. fluocinolon
18. mometazone
19. budesonide
20. fluticazone
21. metyrapone
androgen - Correct Answers -22. testosteron-undecanoat
, antiandrogen - Correct Answers -23. bicalutamide
24. finasteride
anabolic drug - Correct Answers -25. nandrolon
cPDE-5 inhibior - Correct Answers -28. sildenafil
estrogen and anti-estrogens - Correct Answers -Estrogens, synthetic estrogens have
good oral bioavailability.
29. ethynylestradiol -steroidal estrogen
30. estradiol-natural estrogen (premann is natrual, taken from male urine)
Use: for Female hypogonadism (ex.turners syndrome)
-hormone replacement therapy
-oral contraceptive
-in males BPH
-for urinary bleeding, acne
Side effects: increased cancer risks
-hyperplastic changes in breasts
-at high doses increased blood coagulation
to avoid side effects inject IV or transdermally
Estrogen receptor modulators
31. clomifen (fertillity pill) decreases feedback inhibition causing a FSH and LH surge
which triggers ovulation and pregnancy
Selective estrogen R modulators (SERMS)
32. tamoxifen -partial competitive agonist of Estrogen R, but in the presence of high
estrogen levels blocks so it is perfect for estrogenlevel induced breast cancer. possible
increase in endometrial cancer.
33. raloxifen - estrogen agonist for bone, but antagonist for the breast and uterus. used
as a prophylaxis for post meno osteoporosis. No increase in cancer.
Aromatase inhibitor
34. anastrozole - use to treat estrogen dependent post menopausal breast cancer, by
blocking Aromatase from convertin androsterendione to estrone.
GnRH analog
26. goserelin - usually to treat prostate cacinoma, induces the non pulsatile production
of Testosterone and estrogen, thus inducing its negative regulation of it
GnRH Antagonist
27. degarelix-used in the treatment of Prostate carcinoma, prevents binding of GnRH to
its receptor, thus decreasing LH FSH, and thus decreasing Testosterone production.