Pharm 2 Flashcards
Histamine
Biogenic amine
smooth muscle stim, intense vasodepressor, mimics allergic and hypersensitivity reactions.
physiological - gastric acid secretion, neuromodulation and neurotransmission
histamine synthesis
histidine decarboxylase takes histidine (AA) to histamine
histamine degredation
2 steps - histamine methyltransferase and MAO
Cells which produce histamine
Mast cell pool - slowly sun largest supply of histamine
-mast cells and basophils
released in shock or allergic reaction.
GI, Skin, CNS - rapidly syn and works as a neurotransmitter
H-1 receptors
classical smooth muscle, vascular effects
- constriction of bronchi, gut, smooth muscle and large blood vessels
- largest effect at microvasculature»_space; dilation of arterioles and drop in BP and increase cap perm»_space; edema
H-2 receptors
found in GI tract - mediate gastric secretion of HCL
H-3 receptors
inhibition of adenyl cyclase through Gi protein
CNS H receptors
H-3 and H-1
HIstamine in rodents
arteriole CONSTRICTION
histamine in rabbits
pronounced vessel constriction, increased BP
Cromolyn
blocks mast cell degranulation - used as prophylaxis for bronchial asthma in people
H-1 antihistamines
orally absorbed in mono gastric animals, can give IM
competitive inhibitors - most effective as a prophylactic
H-1 antihistamines side effects
CNS - sedation
Anti-cholinergic - dry mouth, blurred vision, tachycardia
contraindications - glaucoma, ileus, cardiac arrythmias
anaphylactic reaction treatments
- systemic epinephrine - physiological antagonism - bronchial dilation and vasoconstriction
- Fluids
- adjunctive - H-1 antihist > Benadryl, Corticosteroids
Treatment of dermal conditions
-uticaria, hypersensitivity reactions, insect stings, pruritus
H-1 antihistamines - systemically or topically