PreOperative Medications - Lecture 1/29/24 Flashcards
If histamine is released what receptor/receptors do we target with antagonists?
Both the H1 and H2 receptors
What drugs induce histamine release?
Morphine
Mivacurium (not available in USA)
Pancuron - in high doses
Protamine (heparin)
Atracurium (Tracrium)
What happens when histamine activates H1?
Hyperalgesia & inflammatory pain.
What happens when histamine activates H2?
Elevates CAMP (B1-like stimulation)
Increases acid/volume production in stomach
What does H1 activate?
Muscarinic, cholinergic, 5-HT3, & Alpha adrenergic receptors
What does H2 activate?
5-HT3 and B1
What are the signs of H1 & H2 activation by histamine?
Hypotension d/t release of NO
Capillary permeability
Flushing
Prostacyclin release
Tachycardia
How does an anti-histamine work? Does it prevent histamine release?
No, works by preventing or limiting the responses to the histamine release. Prevents reactions/effects of histamine on the receptor - has to compete with the inverse agonists.
What is Benadryl mainly used for?
Antipruritic
What is the E 1/2 time of Benadryl?
7-12 hours
What is the Oculo-emetic reflex? What H1 receptor antagonist is used to prevent this reflex? How does the drug prevent the reflex?
The oculo-emetic reflex causes increased nausea and vomiting due to extensive manipulation of extraocular muscles
Prevent with Benadryl
Inhibits the afferent arc of the oculo-emetic reflex.
What are the black box warnings for Phenergan? What years did they come out?
2005 - Respiratory arrest in children under 2
2009- Infiltration causing serious necrosis
What diseases are H2 antagonists primarily used in?
Duodenal Ulcers
GERD
What is the major side effect of H2 antagonist?
Weakend gastric mucosa d/t bacteria b/c stomach not acidic enough to kill off bacteria leading to increased pulmonary infections and candida albicans overgrowth. Usually seen with chronic OTC use.
By how much can a H2 antagonist increase serum creatinine? Why does this happen?
Increases by 15% b/c there is competition for tubular secretion
Name examples of H2 antagonists
Cimetidine (Tagamet)
Ranitidine (Zantac)
Famotidine (Pecid)
Which H2 antagonist STRONGLY inhibits CYP450? What drugs last longer because of this?
Cimetidine
Warfarin, Phenytoin, Lidocaine, TCAs, Propranolol, Nifedipine, Meperidine, Diazepam
Name the 2 major adverse effects of Tagamet
Increased levels of prolactin (men develop boobs)
Inhibits dihydrotestosterone binding to androgen receptors causing impotence
Which H2 antagonist has a weaker binding to CYP enzymes & no significant interactions with other drugs?
Zantac