Study Cards Flashcards
Beta-2 Adrenergic Receptors
- G protein coupled receptor that is coupled to the Gs protein
- Activated by Epinephrine & Norepinephrine
When Stimulated:
- Increase Heart Rate
- Increase Contractility (inotropic effect)
- Increased Lipolysis
- Increased Insulin Secretion
- Increased Aqueous Humor Production
- Ciliary Muscle Relaxation (smooth muscle in eye)
- Vasodilation
- Bronchodilation
- Decreased Uterine Tone
Beta-1 Adrenergic Receptors
*G-Protein-coupled receptor associated with the Gs subunit
Stimulation causes:
- Increased Heart Rate
- Increased Contractility
- Increased Renin Release
- Increased Lipolysis
Alpha-1 Adrenergic Receptor
- G protein coupled receptor associated with the Gq subunit
- Activated by Epinephrine & Norepinephrine
Stimulation causes:
- Increased Vascular Smooth Muscle Contraction
- Increased Pupillary Dilator Muscle Contraction
- Increased Intestinal & Bladder Sphincter Muscle Contraction
Alpha-2 Adrenergic Receptors
- G protein-coupled receptor associated with the Gi subunit
- Epinephrine and Norepinephrine signal through this receptor where it inhibits the release of norepinephrine in a form of negative feedback
Stimulation causes:
- Decreased Sympathetic Outflow
- Decreased Insulin Release
- Decreased Lipolysis
- Increased Platelet Aggregation
- Decreased Aqueous Humor Production
P450 Inhibitors
Decrease the activity of the P450 enzyme, impairing the metabolism of drugs that are metabolized by the P450 system
Quinidine Ciprofloxacin Isoniazid Grapefruit Juice Acute Alcohol Use Erythromycin (Macrolide) Indinavir Cimetidine Sulfonamides Ketoconazole Amiodarone
P450 Inducers
Increase the activity of the P450 enzymes causing drugs that are metabolized by P450 to be metabolized at an increased rate.
Higher doses of medications may be needed to maintain therapeutic levels
Griseofulvin Phenytoin Carbamazepine Rifampin Barbiturates Chronic Alcohol Use St. John's Wart
Benzodiazepine Antidote
Flumazenil
-Reverses the effects of benzodiazepines by competitive inhibition at the benzodiazepine binding site on the GABA receptor
Warfarin Antidotes
Vitamin K
-helps reverse the anticoagulation effects but does not have immediate onset of action
Fresh Frozen Plasma
-replaces coagulation factors and helps to reverse warfarin effects more quickly than vitamin K
Beta Blocker Antidote
Glucagon
-Increases intracellular cAMP and cardiac contractility
Opioid Antidote
Naloxone
- U-opioid receptor antagonist
- Used in acute life-threatening opioid toxicity
Naltrexone
- Opioid receptor antagonist
- Used for dependence treatment rather than in emergent treatment of overdose
Dinoprostone & Misoprostol
Prostaglandins that act to ripen the cervix Indications: -Promote cervical ripening -Prevent GI ulcers -Medical abortion
Side Effects:
- Fetal Distress
- Hyperstimulation of Uterus
Vaginal insertion before induction of labor (oxytocin) to soften the cervix
Clomiphene
Used for ovulatory dysfunction. Selective estrogen receptor modulator (SERM), acts as an antagonist in the hypothalamus. Indications: -Infertility -PCOS Mechanism of Action -Estrogen Antagonist -Increases GnRH, LH, and FSH Secretion -Induction of Ovulation Side Effects -Multiple Gestations -Visual Disturbances -Hot Flashes
Opioid Indications
- Pain
- Weaning (Methadone)
- Cough (Codeine)
- Diarrhea (Loperamide & Diphenoxylate)
Opioid Mechanism of Action
- Interacts at the mu (u), kappa (K), and delta receptors.
- Decrease synaptic transmission- open K+ channels & close CA2+ channels
- Inhibit release of acetylcholine, norepinephrine, 5-HT, glumate, & substance P
Opioid Side Effects
- Respiratory Depression
- Addiction
- Miosis (pinpoint pupils)
- Constipation