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
Serotonin agonist ergots
Erogotamine
Dihydroxyergotamine
Methysergide
Oxytocin agonist ergots
Ergometrine/Ergonovine
Dihydrergometrine
Methyl ergometrine/Methergin
Miscellaneous ergots
Ergotoxine
LSD/ Ly Sergic Diethylamide
Drugs causing pulmonary fibrosis
Bleomycin
Amiodarone
Doxycycline
Nitrofurantoin
Ergots
Sulfonamides
Talc
acute migraine attack
unilateral pulsatile headache
mild headache- NSAIDs (Paracetamol, Aspirin, Indomethacin, Nefopam) + caffeine
moderate to severe headache - Triptans > erogotamine
if triptans are contraindicated, opioids (iv morphine or pethidine, nasal spray of butarphanol)
aura
antiemetics (domperidone, methoclopramide)
Antipsychotics( Chlorpromazine, Prochlorperazine)
Prophylaxis in chronic migraine
- beta blockers - Propranolol
- antiepileptics - valproate, topiramate, gabapentin
- calcium channel blockers- flunarizine, verapamil
- TCA- antitryptilene, nortriptyline
- antiserotonin - cyproheptadine, ketanserin, methysergide
- mao inhibitor - phenelzine
off label use- petasite plant, Clonidine, botulinum toxin
new drug- cgrp 2 inhibitor
cgrp 2 inhibitor
oral
1. rimegepant
2. atogepant
3. olcegepant
4. zavegepant
mab against gcrp2(inj)
1. erenumab
2. eptinezumab
3. galcanezumab
4. fremanezumab
5HT2
5HT 2C agonist - Lorcaserin
5HT 2A/B/C antagonist - Olanzapine, Clozapine
5HT2 to 4 antagonist - Cyproheptadine, Ketanserin, Methysergide
5HT3 antagonists
antimotility in GIT - alosetron for treatment of diarrhoea in IBS
antiemetics in CTZ -doc for chemotherapy induced nausea and vomiting, radiotherapy induced nausea vomiting, gastroenteritis
- Ondesetron (emset), Granisetron, Tropisetron, Ramosetron, Palonosetron (longest, most potent)
antiemetics
- motion sickness - antimuscarinic (hyoscine), antihistaminic (diphenhydramine, promethazine) - not effective in CINV RINV gastroenteritis
- CINV, RINV, gastroenteritis - 5HT3 antagonist, D2 antagonist, NK1 antagonist , CB1 agonist - not effective in motion sickness
CINV
- doc - setrons - Ondesetron, Granisetron, Palonosetron - only effective upto 24 hrs
- Pitants - block NK1 - Aprepitant, Fosaprepitant, Netupitant, Rolapitant
- D2 antagonist - Domperidone, Methoclopramide
- CB1 agonist - Nabilone, Dronabinol
- Dexamethasone (glucocorticoid)
setron effective in delayed phase also
Palonosetron
setron effective in delayed phase also
Palonosetron
antiemetic which stimulates appetite
Nabilone
Dronabinol
CB1 inverse agonist
Rimonabant (supresses appetite - antiobesity drug)
banned- suicidal thought
THT4 antagonist
Cisapride - banned
Mosapride
Tegaserod - banned
Renzapride
Itopride
Prucalopride
Prokinetics
- contract LES - treatment of GERD and to prevent aspiration into lung
- increase gastric motility - used in gastroparesis
- increase intestinal motility - used in constipation
Prokinetics list
- 5HT4 agonist - Mosapride, Itopride, Prucalopride
- D2 antagonist - Domperidone
- Anticholinesterase - Neostigmine
- All above action - Methoclopramide
which antiemetic can cause Parkinson and hyperprolactinemia
Methoclopramide
which antibiotic has prokinetic action
Erythromycin (stimulates motilin receptor)
inhibit Phospholipase A2
corticosteroid
inhibit COX enzyme
NSAID
inhibit LOX enzyme
Zileuton
dual COX and LOX inhibitor
Licofelone - treatment of osteoarthritis
inhibitor of PAF
Apafant
Lexipafant
Modipafant
treatment of acute pancreatitis
PGE1 (synthetic form)
- Gemeprost (vaginal) - MTP
- Lubiprostone (oral) - chloride secretor used in constipation in IBS
- Alprostadil(iv) - vasodilator - erectile dysfunction (cavernosal inj), open ductus arteriosus, critical limb ischemia
- Misoprostol - MTP upto 63 days/1st trimester (sublingual/vaginal) , treatment of NSAID induced peptic ulcer (oral)
SE- diarrhoea, teratogenic (mobius syndrome)
MTP/ Medical abortion
PGE1 - Misoprostol, Gemeprost (1st trimester)
PGE2 - Dinoprostone (2nd)
PGF2alpha - Dinoprost, Carboprost (2nd)
antiprogestin - Mifepristone
antifolate - Methotrexate (no longer used for MTP as it causes incomplete abortion)
MTP guidelines in India
day 1- Mifepristone 200 mg oral (kills fetus)
day 3- Misoprostol (expels fetus)
upto 49 days of gestation (400 microgram orally or vaginally)
upto 63 days of gestation (800 microgram sublingual or vaginally)
PGE2
Dinoprostone
DOC for cervical ripening (dilated) - vaginally
MTP (2nd trimester)
SE- osteoporosis
PGF 2 alpha
Dinoprost - MTP 2nd trimester - iv or intraamniotic
Carboprost - MTP 2nd trimester (im inj) and controls post partum haemorrhage (im)
SE-asthma
Latanoprost, Bimatoprost, Travoprost, Tafluprost - topical eye drops used as DOC for glaucoma
PGI2/prostacyclin
Treprostinil
Iloprost
Epoprostinol
iv
Doc for pulmonary artery hypertension
antiplatelet during hemodialysis
TXA2
physiological antagonist of PGI2
