Pharmacology Final Flashcards
Minimum effective concentration
The minimum amount of drug required for drug effect.
Nitrites
The first agents used to relieve angina.
Finasteride
Used to treat BPH only in men without large postvoid residuals. Inhibits conversion of testosterone to DHT. Can treat male pattern baldness. Results require continued tx-reversal of effects within one year if discontinued. Follow the aptient every 1-3 months. Avoid drugs that can cause urinary retention such as anticholinergics, antihistamines, and decongestants. Women of childbearing age must not handle crushed or broken tablets due to possible absorption and risk to male fetuses.
Drug Development
Drug discovery and manufacturing takes 10-12 years with a cost of more than $1 billion for each drug. Out of every 5000 to 10000 compounds that begin preclinical testing only one makes it through the FDA approval process.
Drug Inclusion and Exclusion
Inclusion: persons between ages 18 and 65, 50-100 kg, stable dose of cardiac medications, and no-added-salt diet
Exclusion: pregnant/nursing, childbearing age, symptomatic cardiac disease, hepatic dysfunction, chronic kidney disease, neurologic disorders, musculoskeletal disorders. Persons with clinically significant abnormal laboratory values.
Drug discover and development
Drug target - basic research, preclinical and animal assays, clinical development-phase 1 - 20-100 healthy volunteers, phase 2 100-300 patients - safety and efficacy - dose optimization, phase 3 - 1000-5000 patients-large scale studies-efficacy and side effects
Pharmcokinetics
The process of drug movement throughout the body necessary to achieve drug action
Pharmcodynamics
Mechanisms of action and effects of a drug on the body; includes onset, peak, and duration of effect on a drug
Bioavailability
The percentage of administered drug available for activity
Therapeutic index
The relationship between the therapeutic dose of a drug and the toxic dose of a drug
Albuterol
High doses or overuse of beta 2 adrenergic agonists can cause some degree of beta 1 response such as nervousness, tremor, and increased pulse rate. Albuterol is one that has a rapid onset of action, longer duration and of action, and few side effects. Treatment of asthma with side effects such as ataxia, headache, nasopharyngitis, insomnia, weakness, dry mouth, nausea, diarrhea, edema, urinary retentions, muscle cramps, hyperhidrosis. Hyperglycemia, hypokalemia, infection, chest pain, dyspnea.
Pediatric Drug Considerations
Family centered care, developmental and cognitive differences. Lack of maturation in GI tract in infancy. Gastric pH is alkaline at birth-favors alkaline drugs. Gastric emptying and GI motility are unpredictable in neonates and infants until 6-8 months of age. Reduced surface area of intestines. Increased amount of water which results in lower drug concentration. Decreased protein and fewer receptor sites.
Geriatric Drug Considerations
Reduced total body water, lean body mass, reduction in kidney and liver mass, decline in physiologic processes. Adherence, polypharmacy.
Hydrochlorathiazide
Thiazides are used to treat hypertension adn peripheral edema. Do not use if the patient has renal disorders. Promote loss of sodum, potassium, and magnesium. Hypercalcemia may result. Hyperglycemia can also occur. Hyperuricemia. Hyperlipidemia. Dizziness, headache, nausea, vomiting, constipation, and blood dyscrasias. Hypokalmiea which enhances the action of digoxin-toxicity include bradycardian, nausea, vomiting, and visual changes. Enhances the action of lithium.
Insulin
Used to control type 1 diabetes mellitus to lower blood glucose and promotes use of glucose by body cells. Lispro 15-30 mins, peak: 30-90 mins, duration 3-5 hours, regular- onset 30 mins, peak: 1.5-3.5 hours, duration 4-12 hours, NPH: onset-1.5 h, peak 4-12 h, duration: 14-24 h, Glargice: onset: 1-1.5 h, peak: none, duration 24 h+
Digoxin
Inhibits sodium ATPase, promoting increased force of contraciton, cardiac output, and tissue perfusion, decreases ventricular rate. Side effects: anorexia, nausea, vomiting, abdominal pain, headachea, blurred or yellow vision, dizziness, weakness, confusion, visual impairment, depression, anxiety. Bradycardia, bowel necrosis, palpitations, dysrhythmias, thrombocytopenia.
Alpha blockers
Vasodilator, decreased blood pressure. Treat hypertension in patients with lipid abnormalities. Do not affect glucose metabolism. Ex: phenoxybenzamine and phentolamine. Selective: prazosin, terazosin, doxazosin - used to treat BPH. Side effects: dizzinesss, fainteness, lightheadedness, and increased heart rate with first dose, nausea, headache, drowsiness, nasal congestion caused by vasodilation, edema, and weight gain. Reflex tachycardia with phentolamine- decrease in BP, nasal congestion caused by vasodilation and GI distrubance.
Atropine
Anticholinergic. Preoperative medication to reduce salivation, increase heart rate for bradycardia, neuromuscular blockade reversal, cholinergic crisis and dilate pupils for ocular diagnostic examinations. Inhibits acetylcholine by occupying the receptors; increased heart rate by blocking vagus stimulation; promotes pupil dilation by blocking iris sphincter muscle. Side effects: drowsiness, dizziness, nausea, dry mouth, headache, confusion, insomnia, amnesia, constipation, flushing, hypohydrosis, blurred vision, mydriasis, anxiety, photophobia, palpitations, urinary retention, hyperreflexia, ataxia, weakness, dehydration, injection site reaction. Tachycardia, paradoxical bradycardia, hypertension, hypotension, angina, dyspnea, pulmonary edema, respiratory depression, ileus, seizures, dysrhthmia, laryngospasm, coma.
Benztropine
Anticholinergic. To decrease involuntary symptoms of parkinsonism or drug-induced parkinsonism. Blocks cholinergic receptors, thus decreasing acetylcholine to reduce excess cholinergic activity, also blocks dopamine reuptake to prolong dopamine effects and decrease involuntary movement. SE: nausea, vomiting, dry mouth, constipation, anhidrosis, dizziness, headache, drowsiness, blurred vision, confusion, depression, hallucination, weakness, hyperthermia, and paresthesia, mydriasis, urinary retention.
Bethanechol
Cholinergic. To treat urinary retention and neurogenic bladder. Stimulates the cholinergic (muscarinic) receptors; promotes contraction of the bladder; increases GI secretions and peristalsis, pupillary constriction, and bronchoconstriction. SE: nausea, vomiting, diarrhea, abdominal cramps, hypersalivation, diaphoresis, headache, dizziness, flushing, urinary urgency and frequency, weakness, miosis, lacrimation. Tachycardia and hypotension. Bronchospasm, wheezing, and seizures.
Metoclopramide
Suppresses emesis by blocking the dopamine receptors in the CTZ. It is used in the treatment of postoperative emesis, cancer chemotherapy, and radiation therapy. High doses can cause sedation and fatigue. With this agent, the occurrence of extrapyramidal symptoms is more prevalent in children than in adults. Metoclopramide should not be given if the patient has GI obstruction, hemorrhage, or perforation.
Neostigmine (short acting)
Acetylchoinesterase inhibitor. Used for treatment of myasthenia gravis and for neuromuscular blockade reversal and the diagnsosis of MG. May cause dizziness, headache, nausea, vomiting, bradycardia, hypotension, tachycardia, muscle cramps, seizures, and dyspnea.
Edrophonium (short acting for diagnosis purposes)
Cholinesterase inhibitors. Neuromuscular blockade reversal and to diagnose myasthenia gravis. Monitor pulse, respiratory rate, BP, neurologica static, and ECG. May cause diplopia, hypersalivation, dysphonia, dysphagia, dysarthria, diaphoresis, bradycardia, hypotension, respiratory depression, and seizures.
MAOIs
The enzyme monoamine oxidase inactivates norepinephrine, dopamine, epinephrine, and serotonin. By inhibiting MAO the levels rise. Inactivates dopamine in the brian. Tranylcypromae sulfate, isocarboxazid, selegiline HCl, and phenelzine sulfate. Used for depression. Hypertensive crisis can occur with CNS stimulants, sympathomimetics, vasocontrictors, cold medications, phenylephrine, psudoephedrine, tyrame: aged cheese, cream, yogurt, coffee, chocolate, bananas, raisins, italian green beans, liver, pickled foods, sausage, soy sauce, yeast, beer, and red wines. Monitor BP. SE: insomnia, orthostatic hypotension, and anticholinergic effects.
MAOIs
The enzyme monoamine oxidase inactivates norepinephrine, dopamine, epinephrine, and serotonin. By inhibiting MAO the levels rise. Inactivates dopamine in the brian. Tranylcypromae sulfate, isocarboxazid, selegiline HCl, and phenelzine sulfate. Used for depression. Hypertensive crisis can occur with CNS stimulants, sympathomimetics, vasocontrictors, cold medications, phenylephrine, psudoephedrine, tyramine: aged cheese, cream, yogurt, coffee, chocolate, bananas, raisins, italian green beans, liver, pickled foods, sausage, soy sauce, yeast, beer, and red wines. Monitor BP. SE: insomnia, orthostatic hypotension, and anticholinergic effects.
Aspirin
Salicylate. Prostaglandin inhibitor that decreases the inflammatory process. Blood clotting is decreased. Side effects: anorexia, dyspepsia, nausea, vomiting, diarrhea, constipation, abdominal pain, heartburn, and flatulence. Reye syndrome, Steven’s Johnson syndrome, blood dycrasias.
Cephalosporins
Beta-lactam structure and act by inhibiting the bacterial enzyme necessary for cell-wall synthesis. A major antibiotic group used in hospitals and in health care offices. Effective against most gram-positive and some gram-negative bacteria. Examples: cefadroxil, cefaclor, cefixime, cefepime, ceftolozane and toazobactam.
Alpha Agonist
Decrease the sympathetic response from the brainstem in the peripheral vessels. They stimulate the alpha receptors which in turn decreases sympathetic activity; increases vagus activity; decreases cardiac output; and decreases serum epinephrine, norepinephrine, and renin release. Methyldopa, clonidine, and guanfacine. Can cause sodium and water retention-administered with diuretics. Drowsiness, dry mouth, dizziness, and slow heart rate. Do not use with impaired liver function. Restlessness, tachycardia, tremors, headache, and increased BP.
Celecoxib
COX-2 inhibitor
Tetracyclines
First antibiotic effective against gram-positive and gram-negative bacteria. Inhibit bacterial protein synthesis and have a bacteriostatic effect. Treat H.pylori and acne. Take on an empty stomach 1 hour before or 2 hours after mealtime. Side effects: GI disturbances, photosensitivity, do not take during pregnancy, do not take if younger than 8 years of age - irreversibly discolors the permanent teeth. Minocycline can cause damage to the vestivular part of the inner ear, which may result in difficulty maintaining balance. Nephrotoxic when given in high doses. Superinfection. T
TB treatment
Isoniazid is used to treat active tuberculosis and as a prophylactic measure against tuberculosis. SE: drowsiness, tremors, rash, blurred vision, photosensitivity, tinnitus, dizziness, nausea, vomiting, dry mouth, constipation, diarrhea with oral solution, injection site reaction. Blood dyscrasias. Pyridoxine may be prescriped to avoid vitamin B deficiency and to minimize peripheral neuropathy. Treatment lasts 6-9 months and can include rifampin, ethambutol, and pyrazinamide in combination to reduce the bacterial resistance. Hepatotoxicity! Hyperglycemia, ocular toxicity, hyperkalemia, hypophophatemia, hypocalcemia. Rifampin turns body fluids orange and soft contact lenses may be permanently discolored.
Streptomycin
Antitubercular - aminoglycoside - ototoxic, hepatotoxic, and nephrotoxic. Test renal and liver failure. Baseline hearing assessment. Within 2-3 months of tx you want a negative sputum culture. TB can be passed to the fetus.
Epinephrine
To treat nasal congestion, allergic reactions, anaphylaxis, asthma exacerbation, bronchospasm, angioedema, status asthmaticus, cardiac arrest. Acts on alpha nad beta receptors; promotion of CNS and cardiac stimulation and bronchodilation; strengthens cardiac contraciton, increases cardiac rate and cardiac output; reduces mucosal congestion by inhibiting histamine release, reverses anaphylactic reactions. NOT GIVEN ORALLY. Increases renal vasoconstriction, decreasing renal perfusion and urinary output. SE: hypertension, tachycardia, palpitations, restlessness, tremors, dysrhthmia, dizziness, urinary retention, nausea, vomiting, dyspnea, and pulmonary edema.
Tiotropium
Anticholinergic drug used for maintenance treatment of bronchospasms associated with COPD. This drug is administered by inhalation only with the HandiHaler. Adverse effects: dry mouth, constipation, vomiting, dyspepsia, abdominal pain, depression, insomnia, headache, joint pain, and peripheral edema. Caution with use in those with narrow-angle glaucoma, bladder neck obstruction, renal impairment, cardiac dysrhythmias, breastfeeding, and older adults.
Verapamil
Calcium channel blocker used to treat chronic hypertension, angina pectoris, and cardiac dysrhythmias. Act on the arterioles and the heart. Can cause dizziness, headache, confusion, fatigue, orthostatic hypotension, blurred vision, peripheral edema, erectile dysfunction, nausea, and constipation.
Spirinolactone
Potassium sparing diuretics-weaker than other diuretics. Inhibits aldosterone effects on the distal renal tubules to promote sodium and water excretion and potassium retention. Can cause n/v/d, abdominal cramps, dizziness, headache, confusion, weakness, muscle spasms, paresthesia, dehydration, ataxia, erectile dysfunction. Hyperkalemia, hypomagnesemia, hyponatremia, hypocalcemia, hypovolemia, hyperglycemia, hyperuricemia, orthostatic hypotension, bradycardia, metabolic acidosis/alkalosis. The heart rate is more regular, and the possibility of myocardial fibrosis is decreased. Do not take with ARBs or ACE inhibitors because they will increase serum potassium levels. Pair with hydrochlorothiazide or a loop diuretic.
Psyllium
Bulk forming laxative draws water into the intestine. Defecation takes 8-24 hours and may take up to 3 days. Insufficient fluid intake can cause the drug to solidify in the GI tract, which can result in intestinal obstruction. This group of laxatives does not cause dependence. Can cause anorexia, nausea, vomiting, abdominal cramps, flatulence, diarrhea.
Peptic Ulcer Treatment
H2 blocker: cimetidine, famotidine, and nizatidine. Side effects and adverse reaction include headache, agitation, dizziness, nausea, vomiting, constipation, or diarrhea, pruritus, skin rash, vitamin B12 deficiency, erectile dysfunction, and blood dyscrasias.
PPI: Omeprazole-effective against suppressing gastric acid secretions. Can enhace digoxin, oral anticoagulants, benzodiazepines, and phenytoin because they interfere with liver metabolism.
Pepsin inhibitors: sucralfate - mucosal protective drug combines with protein to form a viscous substance that covers the ulcer and prtects it from acid and pepsin.
Misoprostol - prostaglandin analogue - used to prevent and treat peptic ulcer. Suppress gastric acid secretion and increase cytoprotective mucus in the GI tract. Gastric distress from NSAIDs such as aspirin or indomethacin can benefit.
Antacid- neutralize HCl and reduce pepsin activity. Magnesium can cause diarrhea and aluminum and calcium cause constipation. Sithethicone - an antigas agent is found in many antacids.
Two antibiotics, a PPI, and a bismuth or histamine blocker is recommended.
Famotidine
H2 blocker: cimetidine, famotidine, and nizatidine. Side effects and adverse reaction include headache, agitation, dizziness, nausea, vomiting, constipation, or diarrhea, pruritus, skin rash, vitamin B12 deficiency, erectile dysfunction, and blood dyscrasias. Enhances the effects of oral anticoagulants, theophylline, caffeine, phenytoin, diazepam, propranolol, phenobarbial, and CCB. Do not take with iron.
Lansoprazole
PPI: Omeprazole-effective against suppressing gastric acid secretions. Can enhace digoxin, oral anticoagulants, benzodiazepines, and phenytoin because they interfere with liver metabolism. Take before meals. Caution in hepatic impairment, monitor liver enzymes. Side effects include headache, dizziness, diarrhea, or constipation, abdominal pain, vitamin B12 deficiency, and hypomagnesemia.
Glucocorticoids
Natural cortisol produced by the body and are influenced by ACTH. Cortisone drugs - used to treat inflammatory, allergic, and autoimmune disorders like rheumatoid arthritis, myasthenia gravis, etc. Pred
Glucocorticoids
Natural cortisol produced by the body and are influenced by ACTH. Cortisone drugs - used to treat inflammatory, allergic, and autoimmune disorders like rheumatoid arthritis, myasthenia gravis, etc. Prednisone.
SE: prologned use include increased BGL, cushing’s, sodium and water retention, hypertension, euphora, increased intraocular pressure, peptic ulcers, and growth retardation. Should be tapered. Increase effect of NSAIDS and hypokalemia with diuretics. Barbiturates, phenytoin, and rifampin decrease the effects.
Bethanechol chloride
Parasympathomimetic, stimulates the cholinergic receptors, promotes contraction of the bladder, increases GI secretions and peristalsis, pupillary constriction, and bronchoconstriction. Treats urinary retention and neurogenic bladder. Side effects: n/v/d, abdominal cramps, hypersalivation, diaphoresis, headache, dizziness, flushing, urinary urgency and frequency, weakness, miosis, and lacrimation.
Tolterodine tartrate
Decrease urinary frequency, urgency, and incontinence. Anticholinergic. SE: drowsiness, dizziness, dry mouth, eyes, and skin; headache, blurred vision, confusion, diarrhea, abdominal pain, constipation, dyspepsia, dysuria, fatigue, weight gain, arthralgia, hallucinations, and urinary retention. Can cause tachycardia, chest pain, angioedema.