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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)
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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) 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)
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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 16. fludrocortizone
17. fluocinolon
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18. mometazone
19. budesonide
20. fluticazone
21. metyrapone
androgen 22. testosteron-undecanoat
antiandrogen 23. bicalutamide
24. finasteride
anabolic drug 25. nandrolon
cPDE-5 inhibior 28. sildenafil
estrogen and anti-estrogens Estrogens, synthetic estrogens have good oral bioavailability.
29. ethynylestradiol -steroidal estrogen
30. estradiol-natural estrogen (premann is natrual, taken from male urine)