Antiemetics Flashcards
Emesis…
Vomit reflex - controlled in brainstem on dorsal surface of medulla oblongata.
CINV = Chemotherapy induced N&V.
PONV = Post-op N&V.
Antiemetics targetting Histamine….
Cyclizine - motion sickness.
Cinnarizine - motion, vestibular disorders (Menieres and vertigo).
Promethazine - severe morning sickness.
Histamine target side effects…
Drowsiness & Sedation.
Examples of H3 Antagonists…
Betehistine Hydrochloride = Anti-vertigo: activates H receptors on inner ear bl vessels > vasodilation > permeability > reverses endolymphatic hydrous.
H3 Antagonist Side Effects…
GI disturbances, headaches, rashes, pruritus.
Antiemetics targetting Dopamine…
Phenothiazines - morning sickness, IV oral.
Prochloropromazine - tablet IM
Perphenazine - tablet
Trifluoperazine - tablet
Chlorpromazine - tablet IM
Metoclopramide - penetrates BBB, increase motility in GIT. Oral IV IM.
Domperidone - doesn’t penetrate BBB. migraine / cytotoxic thera`py. induces emesis as contraception. Oral IV.
Dopamine target side effects:
Sedation, hypotension, dystonia, dyskinesia, movement disorders, fatigue, motor restlessness, spasmodic torticollis, oculogyric crises, menstruation disorders, QT prolongation, fatigue.
Antiemetics targetting Serotonin 5HT3…
Ondansetron - CINV PONV. Oral IV IM > GI disturbances and headaches.
Antiemetics targetting Substance P and Neurokinin…
Aprepitant - CINV PONV oral IV.
Eosaprepitant.
Casopitant / Maropitant - motion sickness.
Side effects of P/NK antiemetics…
fatigue, listlessness, constipation/diarrhoea, loss appetite, hiccups, dizziness, ringing ears, dyspepsia, anorexia, asthenia, headaches.
Mechanism of Cannabinoids…
Antagonist of CB receptors, act via opioid receptors in CTZ.
Examples of Cannabinoids…
Marion / Dornabinol - Oral.
Nabilone / Cesamet - mimetic of cannabic HTC, chronic pain therapy.
Side effects of Cannabinoids…
drowsiness, dizziness, dry mouth, mood changes, postural hypotension, hallucinations and psychotic reactions.
Corticosteroids used as antiemetics…
Dexamethasone = CINV. used with Dopamine target or Serotonin targets.
Inducing emesis after overdose / alcohol intoxication…
Syrup of ipecac - alkaloid emetine/cepheline. oral working in 15 mins. irritate gastric mycosa to activate CTZ.
Apomorphine - stimulates CTZ/VC. IM/subcut act in 5-10 mins.
Activated charcoal - absorbent that binds toxins.