Flashcards in Exam 3 Deck (57):
Alpha 1 agonist
Used to treat orthostatic hypotension and urinary incontinance
Prevents NE reuptake in the synapse
Affects DA receptors in the brain
Causes constriction of blood vessels when injected (good local anesthetic at mucosal sites).
Sometimes used during endotracheal intubation through the nose.
Stimulates NE release from sympathetic nerve endings independent of nerve action
Also directly stimulate on adrenergic receptors
Used to treat nasal/bronchial congestion and promote sinus drainage
Alpha 1 agonist
Used to raise BP
Greater reflex bradycardia effect due to no opposition from stimulated Beta 1 receptor
Used in neurogenic shock and to maintain BP during spinal anesthesia
Nasal decongestant, hemorrhoids, pupil dilator
Rarely used for supraventricular tachycardia.
8 Beta blockers
Beta 2 inhibitor (also Beta 1)
Used topically to decrease intraoccular pressure in glaucoma.
Decreases aqueous humor production from the ciliary epithelium.
It is used because it doesn't have a membrane stabilizing effect (local anesthetic action), which you don't want in the eye.
Moderate lipid solubility makes it preferable to Nadolol, which otherwise has similar properties.
Beta 1 antagonist
Shortest half life due to rapid inactivation by esterases in the blood.
Only used in acute, critical cardiovascular conditions when you don't want the effects to be long lasting.
Non selective Beta blocker plus specific alpha 1 blocker
Treats moderate to severe primary hypertension (oral) and in acute hypertensive crises (Intravenous).
Side effects include orthostatic hypotension (alpha blockade) and bronchoconstriction (beta blockade)
Less Raynaud's aggravation than regular beta blockers and less tachycardia than regular alpha blockers.
Non competitive inhibitor of alpha 1 and 2 receptors
Used to prevent severe hypertensive episode during surgical removal of a pheochromocytoma. Given prior to surgery.
Also can be used to treat chronic hypertension in patients with inoperable pheochromocytoma.
Alpha 1 and 2 inhibitor
Used to diagnose pheochromocytoma. Small dose will drop BP a lot if hypertension is due to pheochromocytoma.
Used to prevent hypertension during pheochromocytoma surgery (given during surgery).
Also used to reverse hypertension caused by administration of too much alpha agonist.
Can stop spread of tissue necrosis caused by injection of alpha agonist into soft tissue.
Used to reverse oral soft tissue anesthesia in dentistry.
Selective alpha 1 antagonist
Treats mild to moderate primary hypertension
Treats BPH by relaxing bladder neck, prostatic urethra.
Can also treat Raynaud's. Excessive response to cold/emotional stress.
Treats PTSD nightmares (inhibits central alpha 1 receptors)
Can see severe orthostatic hypotension during first dose.
Some extra cellular fluid retention.
Reflex tachycardia, but not as bad as non selective agents because presynaptic alpha 2s can still exert their feedback inhibition effect.
Selective alpha 1 inhibitors
Same effects as Prazosin, but they have longer halflives so they may be better for long term compliance in chronic hypertension
Specific alpha 1 subtype A inhibitors
Subtype A receptors are found in smooth mm of bladder neck and prostate.
Used to treat BPH with few side effects
May cause abnormal ejaculation
Alpha 1 selective inhibitor
Used to treat BPH
Demonstrates uroselectivity because it accumulates in the prostate.
This makes it more specific than others.
Peripherally acting neuronal inhibitor
Decreases DA and NE uptake into storage vesicles
Decreases overall sympathetic tone
Treats hypertension by lowering cardiac output and peripheral resistance
Side effects: sedation, depression, postural hypotension, Bradycardia, fluid retention. Diarrhea and ulcers due to unopposed parasympathetic input to the gut.
Like reserpine but without CNS effects
Antagonized by tricyclic antidepressants because it must get into nerve terminals via the reuptake pump, which they inhibit.
Mechanism of centrally acting adrenergic neuronal inhibitors
Act on centrally located alpha 2 receptors in vasomotor centers, causing feedback inhibition and decrease of sympathetic output.
They don't have much impact on reflex mediated sympathetic output (for example, they don't often cause significant postural hypertension).
Centrally acting alpha 2 agonist in vasomotor centers.
Must be converted to alpha-methylnorepinephrine to become active (same enzymes as DOPA to NE).
Overall dampening of sympathetic output to CV tissues
Used to treat hypertension during pregnancy.
Side effects: fluid retention, dry mouth, sedation (like most alpha 2 agonists). Also autoimmune induction. Rarely causes liver necrosis or hemolytic anemia.
Direct alpha 2 agonist in the central vasomotor centers.
Available orally or through patch.
Can cause rebound hypertension if treatment is abruptly stopped (not seen in methyldopa).
Also used to treat addiction withdrawal, ADHD, PTSD, hot flashes, and migraine.
Analgesia with spinal injection.
Apraclonidine is used to reduce intraoccular pressure in post op patients.
Centrally acting alpha 2 agonist
Used to treat ADHD
Also treats hypertension without the rebound hypertension and sedation seen with Clonidine.
Act on nicotinic receptors
Agonist at a low dose via depolarization of cell membrane
Antagonist at high dose via desensitization and persistent desensitization.
Acts in CNS, autonomic ganglia (CV and GI), and skeletal muscle.
Mast cell cell membrane stabilizer
Inhalation used as prophylaxis against as asthma attacks, not in acute situations.
Also useful for many allergies
Especially useful for asthma caused by specific allergens.
Leukotriene receptor antagonist
Taken orally to reduce the frequency of asthma attacks
Not as effective as corticosteroids
Don't work well in acute situations.
Monteleukast is also approved for seasonal allergies
Lipoxygenase inhibitor, prevents production of leukotrienes
Taken orally to reduce frequency of asthma attacks
May be toxic to the liver
Taken 4x/day, which is annoying.
7 inhaled corticosteroids used in treating asthma
Monoclonal antibody against IgE
Treats moderate to severe allergic asthma
Methylxantheles (Theophylline, Aminophylline)
Cause bronchodilation and inhibit histamine release from mast cells
Decrease cAMP or block adenosine receptors controlling bronchial tone
Theo is given orally, Aminophylline is more water soluble and given intravenously in acute situations.
Many side effects/toxicities.
Inhibits prostaglandin synthesis in the CNS but not in the periphery
Acts at nerve endings
Not anti inflammatory
Doesn't cause GI irritation
Potential to cause hepatotoxicity
Alternative to opioids
Can cause GI irritation
Used for short term, not long term
Celocoxib, rofecoxib, valdecoxib
Selective COX-2 inhibitors
Anti inflammatory, analgesic
Decreases renal perfusion
Increases platelet aggregation
Celecoxib is the only one still on the market
Sodium channel blocker in nerve endings
Affects small, unmyelinated nerves most
Used regional, spinals, and nerve blocks
Can affect motor function when used invasively (spinals). This may be avoided with lower doses.
Most effective drugs for severe pain
Act as agonists at receptors for enkephalins, endorphins
Also act in the limbic system to uncouple emotional component from physical pain
Can also inhibit impulse transmission in the CNS
Those acting on mu receptors are the most effective but have most potential for abuse
Underutilized due to fear of addiction and legal issues
Don't let these issues keep you from prescribing these to people who need them
Seven mu receptor agonists
Partial agonists and mixed agonists/antagonist analgesics
These are ok for moderate pain, but not good enough for severe pain
Analgesic for severe pain
Long acting, orally effective, doesn't cause euphoria
Stigma due to association with heroin withdrawal
Antidepressant adjuvant used in analgesic combinations
Carbamazepine, gabapentin, pregabalin
Anticonvulsant adjuvants used in analgesic combinations
Used in treatment of neurogenic pain
3 Diarrhetics used to treat hypertension
3 adrenergic neuron blockers used to treat hypertension
Alpha 1 receptor blockers used to treat hypertension
Gets converted to T3 in tissues
Half life is 7 days, administered once per day
Need to monitor TSH and free Thyroxine
Pregnant women may need more
Radioactive beta particle emitter that kills thyroid tissue
Can treat thyroid cancer
Dont give to nursing mothers.
Used to think it caused cancer, now not so much
Inhibits T3/T4 synth by inhibiting iodination reactions and coupling of iodotyrosines
Does not inhibit release of T3/T4 that is already made
Often cause elevation of liver enzymes (ALT)
Pt should be taken off medication gradually
6 hr halflife compared to 1.5 hr HL of PTU
Prevents T3/T4 synth, but not its release
Lower risk of agranulocytosis than PTU
Thionamide, treats hyperthyroidism
For severe disease because it inhibits T3/T4 synth AND inhibits conversion of T4 to T3.
Works quicker because of the conversion inhibition effect.
Better for pregnant pt because it is highly protein bound and wont affect fetus
Inhibitors of T3/T4 synthesis
Also inhibit release of preformed T3/T4
Temporary effects, used with Thionamides
Side effects include rash, salivary gland swelling, sore teeth, metallic taste.
Potassium Iodide + Iodide
Protective in case of radioactive iodide exposure
Amino substituted bisphosphonate
Inhibits bone resorption without impairing bone mineralization
Long lasting effects= good for Paget's disease
High doses can cause esophageal erosion
Treats osteoporosis and Paget's
Binds to hydroxyapitite in bone, reduces turnover
Side effect is esophageal erosion
Administered once per year
Inhibits osteoclast activity and induces their apoptosis
Once per month dose
Selective Estrogen Receptor Modulator
Agonist at estrogen receptors in bone, antagonist in breast and uterus
Treats osteoporosis but has risk of venous thromboembolism
1,25 hydroxyvitamin D
Treats osteoporosis and hypoparathyroidism
Increases Ca2+ intestinal absorbtion
Decreases bone resorption, recruits osteoblasts to resorption sites
Marked reduction in fractures
Not dependent of liver/kidneys for activation
Amino substituted bisphosphonate
Treats hypercalcemia of malignancy
Reduced bone pain and fractures in multiple myeloma and metastatic breast cancer
Side effect is osteonecrosis of jaw
Secreted from parafollicular thyroid cells
Lowers Ca2+ by inhibiting osteolysis and increasing Ca2+ excretion by kidney