Exam 3 Flashcards
Midodrine
Alpha 1 agonist
Used to treat orthostatic hypotension and urinary incontinance
Cocaine
Anesthetic
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.
Pseudoephedrine
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
Phenylephrine
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
Acebutolol Atenolol Esmolol Metoprolol Nadolol Pindolol Propranolol Timolol
Timolol
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.
Esmolol
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.
Labetalol
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.
Phenoxybenzamine
Non competitive inhibitor of alpha 1 and 2 receptors
Irreversible
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.
Phentolamine
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.
Prazosin
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.
Doxazosin, terazosin
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
Tamsulosin, siludosin
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
Alfuzosin
Alpha 1 selective inhibitor
Used to treat BPH
Demonstrates uroselectivity because it accumulates in the prostate.
This makes it more specific than others.
Reserpine
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.
Guanethidine
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).
Alpha-methyldopa
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.
Clonidine
Direct alpha 2 agonist in the central vasomotor centers.
Treats hypertension
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.
Guanfacine
Centrally acting alpha 2 agonist
Used to treat ADHD
Also treats hypertension without the rebound hypertension and sedation seen with Clonidine.
Nicotine
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.
Cromolyn sodium
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.
Zafirleukast, Monteleukast
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
Zileuton
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
Beclomethasone Fluisolide Triamcinolone Budesonide Fluticasone Prednisone Mometasone
Omalizumab
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.
Acetaminophen
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
Ketorolac
Injectable NSAID
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 Coronary vasoconstriction Increases platelet aggregation Celecoxib is the only one still on the market
Lidocaine
Local anesthetic 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.
Opioids
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
Morphine Codeine Fentanyl Heroin Hydrocodone Hydromorphone Merperidine Methadone Oxycodone
Partial agonists and mixed agonists/antagonist analgesics
Pentazocine Buorenorphine Butorphanol Tamadol These are ok for moderate pain, but not good enough for severe pain
Methadone
Analgesic for severe pain
Long acting, orally effective, doesn’t cause euphoria
Stigma due to association with heroin withdrawal
Difficult dosing
Amitriptyline
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
Hydrochlorothiazide
Furosemide
Spironolactone
3 adrenergic neuron blockers used to treat hypertension
Reserpine
Methyldopa
Clonadine
Alpha 1 receptor blockers used to treat hypertension
Prazosin
Doxazosin
Terazosin
Levothyroxine
Synthetic T4 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
131I
Radioactive beta particle emitter that kills thyroid tissue
Treats hyperthyroidism
Can treat thyroid cancer
Dont give to nursing mothers.
Used to think it caused cancer, now not so much
Propylthiouracil (PTU)
Methimazole
Thionamides
Treats hyperthyroidism
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
Methimazole
Thionamide
Treats hyperthyroidism
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
Propylthiouracil (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
Iodides
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.
Lugol’s Solution
Potassium Iodide + Iodide
Protective in case of radioactive iodide exposure
Alendronate
Amino substituted bisphosphonate
Treats osteoporosis
Inhibits bone resorption without impairing bone mineralization
Long lasting effects= good for Paget’s disease
High doses can cause esophageal erosion
Risedronate
Pyridinal bisphosphonate
Treats osteoporosis and Paget’s
Binds to hydroxyapitite in bone, reduces turnover
Side effect is esophageal erosion
Zoledronate
Bisphosphonate
Administered once per year
Inhibits osteoclast activity and induces their apoptosis
Ibandronate
Bisphosphonate
Once per month dose
Raloxifene
Selective Estrogen Receptor Modulator
Agonist at estrogen receptors in bone, antagonist in breast and uterus
Treats osteoporosis but has risk of venous thromboembolism
Calcitrol
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
Pamidronate
Amino substituted bisphosphonate
IV only
Treats hypercalcemia of malignancy
Reduced bone pain and fractures in multiple myeloma and metastatic breast cancer
Zoledronate
Bisphosphonate
Treats hypercalcemia
Side effect is osteonecrosis of jaw
Calcitonin
Secreted from parafollicular thyroid cells
Lowers Ca2+ by inhibiting osteolysis and increasing Ca2+ excretion by kidney
3 Drugs that treat Paget’s Disease
Calcitonin, alendronate, Zoledronic acid
