Autacoids Flashcards
Histamine receptors: H1R
Distribution: airway smooth muscle
Post receptor mechanism: Gq, ⬆️IP3, DAG
Function: ⬆️pruritus, pain, bronchoconstriction
Histamine receptor: H2R
Distribution: GI mucosa, heart muscle, mast cell
Post receptor mechanism: Gs, ⬆️ CAMP
Function: gastric acid production
Histamine receptor: H3
Distribution: brain
Post receptor mechanism: Gi, ⬇️CAMP
Function: ⬆️pruritus
Histamine receptor: H4R
Distribution: CD4 T cells
Post receptor mechanism: Gi, ⬇️ CAMP
Function: ⬆️pruritus
H1 blocker effects
Sedation
Anti nausea anti emetic
Anti muscarinic
Anti parkinson
Chlorphenamine
Paradoxical cns stimulation in children
Diphenhydramine, clemastine
Marked sedation, anti motion sickness
2nd generation h1 blockers
Cetirizine Fexofenadine Loratadine Desloratadine Ebastine Levocabastine Azelastine Olopatadine
PK of h1 blockers
Most are well absorbed orally
Peak 1-3 hrs after administration
Indications for antihistamine
Allergic rhinitis Allergic conjunctivitis Urticaria Atopic dermatitis Prophylaxis anti motion sickness
Adverse effects anti histamine
Cns depressive: fatigue, weakness
Cns stimulating: insomnia, irritability
Dry mouth
Less gi motility
Astemizole and terfenadine
⬆️QT interval (torsades de pointes)
Serotonin
Metabolized by MAO
Regulation of mood, sleep, temp control, vomitting, pain perception
Source of ergot alkaloid
Claviceps purpurea
Ergot alkaloids toxicity
Gi: diarrhea, vomitting
Vasoactive peptides: constrictors
Angiotensin 2 Vasopressin Endothelin Neuropeptide y Urotensin
Vasoactive peptide dilators
Bradykinins Natriuretic peptide Vasoactive peptide Substance p Neurotensin Calcitonin gene related peptide
Which angiotensin receptor has affinity for losartan?
AT 1
AT 1 site
Vascular tissues
AT 2 site
Fetal tissues
Moa of ACE INHIBITORS
Blocks conversion of ang 1 to ang 2
Aliskiren moa
Inhibit renin action on angiotensinogen
Maintain Patency of ductus arteriosus in cyanogic congenital heart disease
Alprostadil
Cytoprotective for peptic ulcer
Misoprostol
Open angle glaucoma
Latanoprost
Pulmonary hpn
Epoprostenol
Buspirone
Anxiety, depression
Sumatriptan
Acute migraine
Phenoxybenzamine
Pheomochromocytoma
Cyproheptadine
Carcinoid syndrome
Ketanserin
Hpn
Ondansetron
Prevention of nausea and vomitting in surgery and cancer chemo
Cisapride
Gerd
Tegaserod
Irritable bowel syndrome and constipation
Bromocriptine
Dopamine
Lower prolactin
Ergonovine
Alpha adrenoreceptor and 5ht2
Control of late uterine bleeding
Ergotamine
5ht2
Migraine
