Basics Flashcards
Amine autacoids
Histamine
Serotonin
Lipid autacoids
Eicosanoids - Prostanglandins, Leukotrienes, Lipoxins
Peptide autacoids
Angiotensin
urotensin
endothelin
natriuretic peptide
bradykinin
gas autacoid
nitrous oxide
which 2nd gen antihistaminic crosses BBB
Cetirizine
has sedative action
least sedative 1st gen antihistaminic which can be given during daytime
Chlorpheniramine
H1 partial agonist
Betahistine
brand name: Vertin
used in treatment of vertigo in benign positional vertigo and meniere’s disease
highly sedative 1st gen antihistaminics
- Promethazine (max sedation, LA, anticholinergic)
- Diphenhydramine (transdermal patch for motion sickness)
- Doxepin (also TCA)
- Doxylamine along with vitamin B6 (safest in pregnancy, DOC for morning sickness)
moderately sedative 1st gen antihistaminics
- Cyclizine, Meclizine (most effective for sea sickness)
- Cinnarizine (also blocks calcium channel on vestibular nerves)
- Cyproheptadine (antihistaminic plus antiserotonin - treatment of serotonin syndrome)
- Pheniramine (avil): cough syrup
least sedative 1st gen antihistaminics
- Chlorpheniramine
- Clemastine
- Tirolidine
least sedative 1st gen antihistaminics
- Chlorpheniramine
- Clemastine
- Tirolidine
2nd gen antihistaminic
- Terfinadine, Astemizole (banned) _ CYP3A4 inhibitor, when combined with Erythromycin or Ketoconazole, Torsades de pointes
- Fexofenadine - active Terfinadine
- Cetirizine (new- Levocetirizine)
- Loratidine - most potent
- Rupatidine - PAF inhibitor
- Ebastine, Acrivastine, Bilastine
Mast cell stabilizer
Ketotifen
Olopatidine
Topical antihistaminic
Azelastine
Levocarbastine
Olopatidine
Ketotifen
Alcaftadine
H2 blockers
- Cimetidine
- Ranitidine
- Famotidine - only non competitive blocker
- Roxatidine
- Nizatidine
- Lafutidine
H3 inverse agonist
Tiprolisant/ Pitolisant for narcolepsy or daytime sleepiness (DOC- Modafinil)
Tryptophan hydroxylase inhibitor
Telotristat for treatment of diarrhoea in carcinoid syndrome
5HT1
5HT 1A - Buspirone, Gepirone - anti anxiety drug
5HT 1B/1D- Triptans, Erogotamine - DOC - acute migraine
5HT 1F- Lasmitidan - acute migraine
Triptans
Sumatriptan - DOC for acute attack of migraine
Eletriptan- most effective
Rizatriptan- rapid or fastest
Frovatriptan- longest
Almotriptan
Naratriptan - max oral
Zolmitriptan
Triptans as nasal spray
Sumatriptan
Zolmitriptan
dopamine agonist ergots
Bromocriptine
Pergolide
Cabergoline