AMBOSS pharm gastric Flashcards
H2 antihistamines? 4
Ranitidine
Famotidine
Nizatidine
Cimetidine
Location of H2 receptors?
Gastric parietal cells (oxyntic cells) Vascular smooth muscle Neutrophils Central nervous system Heart Uterus
Histamine effects on H2 receptors? 3
Increased gastric acid secretion
Positive inotropism and enhanced automaticity
Smooth muscle relaxation leading to vasodilatation
H2 antihistamines. revers or nonrevers?
REVERSIBLE
H2 antihistamines. What G protein?
Gs protein-coupled receptor
H2 antihistamines. effect on cAMP?
↓ adenylyl cyclase activity → ↓ cAMP levels –> ↓ protein kinase A activity → ↓ phosphorylation and activation of H+/K+ ATPase → ↓ gastric acid (H+) secretion
what H2 antihistamine has most side effects?
cimetidine
cimetidine Antiandrogenic effect (via release of prolactin)?
erectile dysfunction, gynecomastia, low libido in men
Cimetidine on CYP450?
Inhibition of cytochrome P450 (CYP2C19) → various drugs interactions, e.g., clopidogrel
Cimetidine due to cross of BBB?
Headaches, dizziness, confusion due to its ability to cross the blood-brain barrier
Cimetidine cross what apart from BBB?
placenta (but is considered safe)
Cimetidine on kidney?
Reduces renal creatinine excretion (along with ranitidine)
when to take H2 antihistamine (daytime)?
H2 blockers need to be taken before dinner.
H2 antihistamine indications?
Anaphylactic shock (together with H1 antihistamines)
Symptomatic treatment of peptic ulcers: reduce the production of hydrochloric acid (less effective than PPIs )
Gastroesophageal reflux disease (GERD)
Gastritis
Zollinger-Ellison syndrome
Relative contraindications of H2 antihistamine?
Pregnancy, since cimetidine is known to cross the placental barrier
Nursing mothers
Children