Pharm 6 Flashcards
MOA of thiazolindinediones
Stimulate PPAR-gamma receptor to regulate CHO and lipid metabolism
SE of Thiazolindinediones
Weight gain, edema, hepatotoxicity (3A4), worsens CHF –> HF, fracture, bladder cancer
Hyperglycemic agent that increases cAMP and results in glycogenolysis, gluconeogenesis, reverses hypoglycemia, also used to reverse severe beta-blocker overdose and smooth muscle relaxation
Glucagon
Available bisphosphonates
Alendronate, etidronate, risedronate, pamidronate, tiludronate, and zoledronic acid
MOA of Bisphosphonates
Inhibits osteoclast bone resorption
Uses of bisphosphonates
Osteoporosis, Paget’s disease, and osteolytic bone lesions, and hypercalcemia from malignancy
Major SE of bisphosphonates
Chemical esophagitis
Bisphosphonates that cannot be used on continuous basis because it caused osteomalacia
Etidronate
Used for prevention of postmenopausal osteoporosis in women
Calcium reguators Bisphosphonates: alendronate, risedronate, ibandronate, Estrogen (HRT-Hormone replacement therapy)
Used especially in postmenopausal women, dosage should be 1500 mg
Calcium
Vitamin given with calcium to ensure proper absorption
Vitamin D
Disease caused by excess ergot alkaloids
St. Anthony’s Fire
Endogenous substances commonly interpreted as histamine, serotonin, prostaglandins, and vasoactive peptides
Autocoids
Syndrome of hypersecretion of gastric acid and pepsin usually caused by gastrinoma; it is associated with severe peptic ulceration and diarrhea
Zollinger-Ellison Syndrome
Generation of antihistamine that has the most CNS effects
First generation due to being more lipid-soluble
Major indication for H1 receptor antagonist
Use in IgE mediated allergic reaction
Antihistamine that can be used for anxiety and insomnia and is not addictive
hydroxyzine (Atarax)
H1 antagonist used in motion sickness
Dimenhydrinate, meclizine, and other 1st generation
Most common side effect of 1st generation antihistamines
Sedation
Lethal arrhythmias resulting from concurrent therapy with azole fungals (metabolized by CYP 3A4) and these antihistamines which inhibit the 3A4 iso-enzyme.
Terfenadine and astemizole (have been removed from the market)
Clinical use for H2 blockers
Acid reflux disease, duodenal ulcer and peptic ulcer disease
Receptors for serotonin (5HT-1) are located
Mostly in the brain, and they mediate synaptic inhibition via increased K+ conductance
Triptan available in parenteral and nasal formulation
Sumatriptan
H1 blocker that is also a serotonin antagonist
Cyproheptadine
5HT2 antagonist mediate synaptic excitation in the CNS and smooth muscle contraction
Ketanserin, cyproheptadine, and ergot alkaloids (partial agonist of alpha and serotonin receptors)
5ht-3 antagonist that has been MOST associated with QRS and QTc prolongation and should not be used in patients with heart disease
Dolasetron
Drug used in ergot alkaloids overdose, ischemia and gangrene
Nitroprusside
Reason ergot alkaloids are contraindicated in pregnancy
Uterine contractions
SE of ergot alkaloids
Hallucinations resembling psychosis
Peptide causing increased capillary permeability and edema
Bradykinin and histamine
