Pharm Prototypes
Estradiol – Prototype Summary
Indications:
Palliation of moderate to severe vasomotor symptoms associated with menopause
Prevention of postmenopausal osteoporosis
Treatment of female hypogonadism, female castration, ovarian failure
Palliation of inoperable and progressing breast cancer and inoperable prostatic cancer
Actions:
The most potent endogenous female sex hormone.
Responsible for estrogen effects on the body.
Pharmacokinetics:
Route: PO
Onset: Slow
Peak: Days
Duration: Unknown
Topical preparations are not generally absorbed systemically.
T1/2: Not known; metabolized in the liver and excreted in the urine.
Adverse Effects:
Corneal changes
Photosensitivity
Peripheral edema
Chloasma
Hepatic adenoma
Nausea, vomiting, abdominal cramps, bloating
Breakthrough bleeding, change in menstrual flow, dysmenorrhea, premenstrual-like syndrome
Cardiovascular events (stroke or other thromboembolic disorders)
Breast cancer
Norethindrone Acetate – Prototype Summary
Indications:
Treatment of amenorrhea
Abnormal uterine bleeding due to hormonal imbalance
Treatment of endometriosis symptoms
Component of some hormonal contraceptives
Actions:
Progesterone derivative
Transforms proliferative endometrium into a secretory endometrium
Inhibits secretion of pituitary FSH and LH, preventing ovulation
Inhibits uterine contractions
Pharmacokinetics:
Route: PO
Onset: Varies
Peak: Unknown
Duration: Unknown
T1/2: Unknown; metabolized in the liver and excreted in the feces and urine.
Adverse Effects:
Venous thromboembolism
Loss of vision
Diplopia
Migraine headache
Rash, acne, chloasma
Alopecia, breakthrough bleeding, spotting, amenorrhea
Fluid retention, edema, increase in weight
Raloxifene – Prototype Summary
Indications:
Prevention and treatment of osteoporosis in postmenopausal patients
Reduction of risk of breast cancer in postmenopausal patients
Actions:
Increases bone mineral density without stimulating the endometrium
Modulates effects of endogenous estrogen at specific receptor sites
Pharmacokinetics:
Route: PO
Onset: Varies
Peak: 4–7 h
Duration: 24 h
T1/2: 27.7 hours; metabolized in the liver and excreted primarily in feces.
Adverse Effects:
Venous thromboembolism
Hot flashes
Skin rash
Nausea, vomiting, vaginal bleeding
Depression, light-headedness
Stroke, pulmonary embolism, high triglycerides, hepatic impairment
Clomiphene – Prototype Summary
Indications:
Treatment of ovarian failure in patients with normal liver function and normal endogenous estrogens
Off-label use for treatment of male sterility
Actions:
Binds to estrogen receptors
Decreases number of available estrogen receptors
Gives hypothalamus a false signal to increase FSH and LH secretion, leading to ovarian stimulation
Pharmacokinetics:
Route: PO
Onset: 5–8 d
Peak: Unknown
Duration: 6 weeks
T1/2: 5 days; metabolized in the liver and excreted in the urine.
Adverse Effects:
Vasomotor flushing
Visual changes
Abdominal discomfort, distention, and bloating
Nausea, vomiting, ovarian enlargement
Breast tenderness, ovarian overstimulation, multiple births
Oxytocin – Prototype Summary
Indications:
To initiate or improve uterine contractions for early vaginal delivery
To stimulate or reinforce labor in selected cases of uterine inertia
To manage inevitable or incomplete abortion
For second-trimester abortion
To control postpartum bleeding or hemorrhage
To treat lactation deficiency
Actions:
Synthetic form which stimulates the uterus, especially the gravid uterus
Causes myoepithelium of lacteal glands to contract, resulting in milk ejection in lactating patients
Pharmacokinetics:
Route: IV
Onset: Immediate
Peak: Unknown
Duration: 60 min
Testosterone – Prototype Summary
Indications:
Replacement therapy in hypogonadism
Treatment of delayed puberty in male patients and certain breast cancers in postmenopausal patients
Prevention of postpartum breast engorgement
Actions:
Primary natural androgen
Responsible for growth and development of male sex organs and maintenance of secondary sex characteristics
Increases retention of nitrogen, sodium, potassium, and phosphorus
Decreases urinary excretion of calcium
Increases protein anabolism, stimulates red blood cell production
Pharmacokinetics:
Route: Buccal
Onset: Slow
Peak: 10–12 h
IM Onset: Slow Peak: 1–3 d
IM cypionate Onset: Slow Peak: 2–4 wk
IM Onset: 3–5 min Peak: Unknown Duration: 2–3 h
T1/2: 1 to 6 minutes; metabolized in tissue and excreted in urine.
Adverse Effects:
Cardiac arrhythmias, hypertension, fetal bradycardia
Nausea, vomiting, uterine rupture, pelvic hematoma
Uterine hypertonicity, severe water intoxication, anaphylactic reaction
Hydroxyprogesterone Caproate – Prototype Summary
Indications:
Reduction of the risk of preterm birth in patients with a single-fetus pregnancy who have a history of singleton spontaneous preterm birth
Not intended for use in patients with multiple-fetus pregnancy or other risk factors for preterm birth
Actions:
Acts as a synthetic progestin
Exact mechanism by which it reduces risk of recurrent preterm birth is unknown
Pharmacokinetics:
Route: Subcutaneous or IM
Onset: Slow
Peak: Days
Duration: Unknown
T1/2: 16 to 19 days; metabolized in the liver and excreted in urine and feces.
Adverse Effects:
Injection-site reactions
Glucose intolerance, fluid retention, depression
Hypertension, thrombosis, breast cancer, liver disease
Sildenafil – Prototype Summary
Indications:
Treatment of erectile dysfunction in the presence of sexual stimulation
Treatment of pulmonary arterial hypertension
Actions:
Inhibits PDE5 receptors
Leads to a release of nitric oxide
Activates cyclic guanosine monophosphate to cause prolonged smooth muscle relaxation, facilitating blood flow into the corpus cavernosum
Pharmacokinetics:
Route: PO
Onset: 15–30 min
Peak: 30–120 min
Duration: 4 h
T1/2: 4 hours; metabolized in the liver and excreted in urine and feces.
Adverse Effects:
Headache, abnormal vision
Flushing, dyspepsia
Urinary tract infection, rash, hypotension, priapism, hearing loss
Captopril – Prototype Summary
Indications:
Treatment of essential hypertension in the extended-release form
Angina and tachyarrhythmias
Actions:
Blocks ACE from converting angiotensin I to angiotensin II
Leads to decrease in BP, decrease in aldosterone production
Small increase in serum potassium levels along with sodium and fluid loss
Pharmacokinetics:
Route: Oral
Onset: 15 min
Peak: 30–90 min
T1/2: 2 hours; excreted in urine.
Adverse Effects:
Allergic reactions, angioedema
Neutropenia, hypotension, tachycardia
Rash, dizziness, headache, gastrointestinal irritation
Digoxin – Prototype Summary
Indications:
Treatment of heart failure
Atrial fibrillation
Actions:
Increases intracellular calcium
Allows more calcium to enter myocardial cells during depolarization
Results in positive inotropic effect (increased force of contraction)
Increases renal perfusion with diuretic effect and decrease in renin release
Negative chronotropic effect (slower heart rate) and slowed conduction through AV node
Pharmacokinetics:
Route: Oral
Onset: 30–120 min
Peak: 2–6 h
Duration: 6–8 d
IV Onset: 5–30 min
Peak: 1–5 h
Duration: 4–5 d
T1/2: 30 to 40 hours; largely excreted unchanged in urine.
Adverse Effects:
Headache, weakness, drowsiness
Visual disturbances, arrhythmias, GI upset
Milrinone – Prototype Summary
Indications:
Short-term treatment of heart failure in patients who have not responded to digitalis, diuretics, or vasodilators
Actions:
Blocks the enzyme phosphodiesterase
Leads to increase in myocardial cell cAMP
Increases calcium levels in the cell, causing stronger contraction and prolonged response to sympathetic stimulation
Directly relaxes vascular smooth muscle
Pharmacokinetics:
Route: IV
Onset: Immediate
Peak: 10 min
Duration: 8 h
T1/2: 2.3 to 3.5 hours; metabolized in the liver and excreted in urine and feces.
Adverse Effects:
Arrhythmias, hypotension
Nausea, vomiting, thrombocytopenia
Pleuritis, fever, chest pain, burning at injection site
Ivabradine – Prototype Summary
Indications:
Treatment of chronic heart failure in stable patients at maximum beta-blocker doses
To prevent rehospitalizations
Actions:
Blocks HCN channels to slow the heart’s pacemaker
Reduces heart rate with no effect on muscle contraction
Pharmacokinetics:
Route: PO
Onset: Rapid
Peak: 1 h
Duration: 6 h
T1/2: 2.5 hours; metabolized in liver and intestines; excreted in urine and feces.
Adverse Effects:
Bradycardia, atrial fibrillation
Hypo/hypertension, luminous phenomena (visual changes)
Sacubitril/Valsartan – Prototype Summary
Indications:
Reduces the risk of cardiovascular death and hospitalization for heart failure in adult patients with chronic heart failure
Treatment of pediatric patients with symptomatic heart failure due to decreased left ventricular function
Actions:
Inhibits neprilysin, which breaks down natriuretic peptides in the body
By blocking breakdown, more sodium and water are lost
Combination with angiotensin II receptor blockade inhibits RAAS effects, leading to decreased cardiac workload, lower vascular volume, lower BP, and fewer heart failure symptoms
Pharmacokinetics:
Route: PO
Onset: 30 min
Peak: 1.5 h
Duration: 12 h
T1/2: 10 hours; Sacubitril is mostly metabolized by esterases, valsartan mostly remains unmetabolized; excreted in urine and feces.
Adverse Effects:
Hypersensitivity, angioedema
Hypotension, hyperkalemia
Cough, dizziness, renal impairment
Lidocaine – Prototype Summary
Indications:
Management of acute ventricular arrhythmias during cardiac surgery or myocardial infarction
Treatment of refractory ventricular arrhythmias
Actions:
Decreases depolarization, decreasing automaticity of ventricular cells
Increases ventricular fibrillation threshold
Pharmacokinetics:
Route: IM
Onset: 5–10 min Peak: 5–15 min
Duration: 2 h
IV Onset: Immediate Peak: Immediate Duration: 10–20 min
T1/2: 10 minutes, then 1.5 to 3 hours; metabolized in the liver and excreted in urine.
Adverse Effects:
Dizziness, lightheadedness, fatigue
Arrhythmias, cardiac arrest
Nausea, vomiting, anaphylactoid reactions, hypotension, vasodilation
Propranolol – Prototype Summary
Indications:
Treatment of cardiac arrhythmias, especially supraventricular tachycardia
Treatment of ventricular tachycardia induced by digitalis or catecholamines
Also used as antihypertensive, antianginal, and antimigraine headache drug
Actions:
Competitively blocks beta-adrenergic receptors in heart and kidney
Has membrane-stabilizing effect
Decreases influence of sympathetic nervous system
Pharmacokinetics:
Route: Oral
Onset: 20–30 min
Peak: 60–90 min
Duration: 6–12 h
IV Onset: Immediate Peak: 1 min
Duration: 4–6 h
T1/2: 3 to 5 hours; metabolized in liver and excreted in urine.
Adverse Effects:
Bradycardia, heart failure
Cardiac arrhythmias, heart block
Cerebrovascular accident, pulmonary edema, gastric pain
Flatulence, nausea, vomiting, diarrhea, impotence, decreased exercise tolerance
Amiodarone – Prototype Summary
Indications:
Treatment of life-threatening ventricular arrhythmias
Actions:
Acts directly on heart muscle cells to prolong repolarization and the refractory period
Increases threshold for ventricular fibrillation
Acts on peripheral smooth muscle to decrease peripheral resistance
Pharmacokinetics:
Route: Oral
Onset: 2–3 d
Peak: 3–7 h
Duration: Prolonged
IV Onset: Immediate
Diltiazem – Prototype Summary (Antiarrhythmic)
Indications:
Extended-release preparation used to treat hypertension and angina in adults
Other preparations used for angina and cardiac dysrhythmias (rapid atrial fibrillation, atrial flutter, paroxysmal supraventricular tachycardia)
Actions:
Blocks movement of calcium ions across cell membrane
Depresses generation of action potentials, delays phases 1 and 2 of repolarization
Slows conduction through AV node
Pharmacokinetics:
Route: Oral
Onset: 30–60 min
Peak: 2–3 h
Duration: 6–8 h
IV Onset: Immediate
Peak: 2–3 min
Duration: Unknown
T1/2: 3.5 to 6 hours; metabolized in the liver and excreted in urine.
Adverse Effects:
Dizziness, lightheadedness
Headache, asthenia, peripheral edema
Bradycardia, AV block, flushing, nausea, hepatic injury
Atorvastatin – Prototype Summary
Indications:
Adjunctive therapy for reduction of elevated cholesterol, triglyceride, and LDL levels
Prevention of myocardial infarction, stroke, and angina in adults with multiple risk factors for heart disease, in patients with heart disease, and in patients with type 2 diabetes
Approved to lower cholesterol in children 10 to 17 years of age with familial hypercholesterolemia after failing diet therapy
Actions:
Inhibits HMG-CoA
Causes decrease in serum cholesterol, triglycerides, and LDL levels
Increases HDL levels
Pharmacokinetics:
Route: Oral
Onset: Slow
Peak: 1–2 h
Duration: 20–30 h
T1/2: 14 hours; metabolized in liver and cells and excreted in bile.
Adverse Effects:
Headache, flatulence, abdominal pain, cramps, constipation
Rhabdomyolysis with acute renal failure, liver impairment, myalgias
Ezetimibe – Prototype Summary
Indications:
Adjunct to diet and exercise to lower serum cholesterol levels
Combination with atorvastatin or simvastatin for treatment of homozygous familial hypercholesterolemia
With diet for treatment of homozygous sitosterolemia to lower sitosterol and campesterol levels
Actions:
Works in small intestine to inhibit cholesterol absorption
Pharmacokinetics:
Route: Oral
Onset: Moderate
Peak: 4–12 h
T1/2: 22 hours; metabolized in the liver and small intestine, excreted in feces and urine.
Adverse Effects:
Headache, dizziness, abdominal pain
Diarrhea, upper respiratory infection, back pain, myalgia, arthralgia, hepatitis or liver dysfunction
Evolocumab (Repatha) – Prototype Summary
Indications:
Reduction of risk of MI, stroke, and coronary revascularization in adults with cardiovascular disease
Adjunct to diet, alone or with other therapies to lower LDL in adults with primary hyperlipidemia
Adjunct to other therapies to lower LDL in patients with homozygous familial hypercholesterolemia
Actions:
Binds to free PCSK9, allowing liver to decrease the blood LDL levels
Pharmacokinetics:
Route: Subcutaneous
Onset: Fast
Peak: Maximum enzyme suppression in 4 h
T1/2: 11 to 17 days; eliminated via binding to PCSK9.
Adverse Effects:
Hypersensitivity effects (rash, urticaria)
Upper respiratory tract infection, nasopharyngitis, influenza
Injection site reactions
Aspirin – Prototype Summary
Indications:
Reduction of risk of death and myocardial infarction in patients with chronic coronary artery disease
History of MI or unstable angina pectoris, or chronic stable angina
Reduction of risk of death and recurrent stroke in patients with an ischemic stroke or transient ischemic attack
Also indicated for analgesic and fever reducer
Actions:
Inhibits prostaglandin synthesis resulting in inhibition of platelet aggregation
Inactivates cyclooxygenase-1 (COX-1), preventing the conversion of arachidonic acid to thromboxane A2
Lack of thromboxane A2 inhibits platelet aggregation
Pharmacokinetics:
Route: Oral
Onset: 5–30 min
Peak: 0.25–2 h
Duration: 3–6 h
T1/2: 15 minutes to 12 hours; metabolized in the liver and excreted in urine.
Adverse Effects:
Acute aspirin toxicity with hyperpnea leading to fever, coma, and cardiovascular collapse
Nausea, dyspepsia, heartburn, epigastric discomfort
GI bleeding, occult blood loss, dizziness, tinnitus, difficulty hearing, anaphylactoid reaction
Heparin – Prototype Summary
Indications:
Prevention and treatment of venous thrombosis and pulmonary embolism
Treatment of atrial fibrillation with embolization
Treatment of disseminated intravascular coagulation (DIC)
Prevention of clotting in blood samples and heparin lock sets
Adjunct in treatment of myocardial infarction and stroke
Actions:
Inhibits thrombus and clot production by blocking conversion of prothrombin to thrombin and fibrinogen to fibrin
Pharmacokinetics:
Route: IV
Onset: Immediate
Peak: Minutes
Duration: 2–6 h
Subcutaneous Onset: 20–60 min Peak: 2–4 h Duration: 8–12 h
T1/2: 30 to 180 minutes; metabolized in cells and excreted in urine.
Adverse Effects:
Bleeding, epidural or spinal hematoma
Heparin-induced thrombocytopenia, hypersensitivity reactions
Loss of hair, bruising, chills, fever, osteoporosis, suppression of renal function with long-term use
Alteplase – Prototype Summary
Indications:
Treatment of myocardial infarction
Acute pulmonary embolism
Acute ischemic stroke
Restoration of function in occluded central venous access devices
Actions:
Acts as enzyme to convert endogenous plasminogen to plasmin
Breaks down fibrin clots, fibrinogen, and other plasma proteins; lyses thrombi and emboli
Pharmacokinetics:
Route: IV
Onset: Immediate
Peak: End of injection
Duration: Unknown
T1/2: 72 minutes; metabolized in plasma; excretion method unknown.
Adverse Effects:
Bleeding, hypersensitivity
Antihemophilic Factor – Prototype Summary
Indications:
Treatment of classic hemophilia to provide temporary replacement of clotting factors
Correct or prevent bleeding episodes or allow necessary surgery
Actions:
Normal plasma protein needed for transformation of prothrombin to thrombin, the final step in the clotting pathway
Pharmacokinetics:
Route: IV
Onset: Immediate
Peak: Unknown
Duration: Unknown
T1/2: 12 hours; cleared from body by normal protein metabolism.
Adverse Effects:
Allergic reaction, stinging at injection site, headache
Rash, chills, nausea
Aminocaproic Acid – Prototype Summary
Indications:
Treatment of excessive bleeding resulting from hyperfibrinolysis
Used to prevent recurrence of subarachnoid hemorrhage
Management of megakaryocytic thrombocytopenia, decrease platelet administration need
Abort and treat attacks of hereditary angioneurotic edema
Actions:
Inhibits plasminogen activator substances
Has antiplasmin activity that inhibits fibrinolysis and prevents breakdown of clots
Pharmacokinetics:
Route: Oral
Onset: Rapid
Peak: 2 h
Duration: Unknown
IV Onset: Immediate Peak: Minutes Duration: 2–3 h
T1/2: 2 hours; excreted unchanged in urine.
Adverse Effects:
Dizziness, tinnitus, headache, weakness
Hypotension, nausea, cramps, diarrhea
Fertility problems, malaise, elevated serum creatine phosphokinase
Epoetin Alfa – Prototype Summary
Indications:
Treatment of anemia associated with chronic renal failure related to HIV infection or chemotherapy in cancer patients
Reduce the need for allogenic blood transfusions in surgical patients
Actions:
Natural glycoprotein that stimulates red blood cell production in the bone marrow
Pharmacokinetics:
Route: Subcutaneous
Onset: 7–14 d
Peak: 5–24 h
Duration: 24 h
T1/2: 4 to 13 hours; metabolized in serum and excreted in urine.
Adverse Effects:
Headache, arthralgias
Fatigue, asthenia, dizziness
Hypertension, edema, chest pain, nausea, vomiting, diarrhea
Deep vein thrombosis, thrombotic events
Ferrous Sulfate – Prototype Summary
Indications:
Prevention and treatment of iron deficiency anemia
Dietary supplement for iron
Actions:
Elevates serum iron concentration
Converted into hemoglobin or stored for eventual conversion to a usable form of iron
Pharmacokinetics:
Route: Oral
Onset: 4 d
Peak: 7–10 d
Duration: 2–4 mo
T1/2: Not known; recycled for use; not excreted.
Adverse Effects:
GI upset, anorexia
Nausea, vomiting, constipation, diarrhea
CNS toxicity progressing to coma, death in overdose cases
Folic Acid – Prototype Summary
Indications:
Treatment of megaloblastic anemia due to folate deficiency, malabsorption, or nutritional deficiency
Prevention of neural tube defects
Actions:
Reduced form of folic acid required for nucleoprotein synthesis and maintenance of normal erythropoiesis
Pharmacokinetics:
Route: Oral, IM, subcutaneous, IV
Onset: Varies
Peak: 30–60 min
T1/2: Unknown; metabolized in liver and excreted in urine.
Adverse Effects:
Allergic reactions, pain and discomfort at injection site
Hydroxocobalamin – Prototype Summary
Indications:
Treatment of vitamin B12 deficiency
Increased vitamin B12 requirements related to disease, pregnancy, or blood loss
Treatment of pernicious anemia
Actions:
Essential for nucleic acid and protein synthesis
Used for growth, cell reproduction, hematopoiesis, nucleoprotein and myelin synthesis
Pharmacokinetics:
Route: IM
Onset: Intermediate
Peak: 60 min
T1/2: 24 to 36 hours; metabolized in liver and excreted in urine.
Adverse Effects:
Itching, transitory exanthema
Mild diarrhea, anaphylactic reaction, heart failure, pulmonary edema, hypokalemia, pain at injection site
Hydroxyurea – Prototype Summary
Indications:
Reduction of frequency of painful crisis and need for blood transfusions in adult patients with sickle cell anemia
Actions:
Increases fetal hemoglobin production in bone marrow
Dilutes formation of abnormal hemoglobin S
Pharmacokinetics:
Route: Oral
Onset: Varied
Peak: 1–4 h
Duration: 18–20 h
T1/2: 3 to 4 hours; metabolized in liver and excreted in urine.
Adverse Effects:
Dizziness, headache
Rash, erythema, anorexia
Nausea, vomiting, stomatitis, bone marrow depression, cancer
Hydrochlorothiazide – Prototype Summary
Indications:
Adjunctive therapy for edema associated with heart failure, cirrhosis, corticosteroid or estrogen therapy, and renal dysfunction
Treatment of hypertension as monotherapy or in combination with other antihypertensives
Actions:
Inhibits reabsorption of sodium and chloride in distal renal tubules
Increases excretion of sodium, chloride, and water by kidneys
Pharmacokinetics:
Route: Oral
Onset: 2 h
Peak: 4–6 h
Duration: 6–12 h
T1/2: 5.6 to 14 hours; metabolized in liver and excreted in urine.
Adverse Effects:
Dizziness, vertigo, orthostatic hypotension
Hypokalemia and other electrolyte alterations
Nausea, anorexia, vomiting, dry mouth, diarrhea
Dehydration, polyuria, nocturia, muscle cramps, spasms
Furosemide – Prototype Summary
Indications:
Treatment of edema associated with heart failure, acute pulmonary edema, hypertension
Actions:
Inhibits reabsorption of sodium and chloride from distal renal tubules and loop of Henle
Leads to sodium-rich diuresis
Pharmacokinetics:
Route: Oral
Onset: 60 min
Peak: 60–120 min
Duration: 6–8 h
IV, IM Onset: 5 min Peak: 30 min Duration: 2 h
T1/2: 120 minutes; metabolized in liver and excreted in urine.
Adverse Effects:
Dizziness, vertigo, paresthesia
Orthostatic hypotension, rash, urticaria
Nausea, anorexia, vomiting, hyperglycemia, hyperuricemia
Urinary bladder spasm, ototoxicity, dehydration, electrolyte disturbances
Acetazolamide – Prototype Summary
Indications:
Adjunctive treatment of open-angle glaucoma, secondary glaucoma
Preoperative use in acute angle-closure glaucoma when delay of surgery is indicated
Edema caused by heart failure; drug-induced edema
Prevention or treatment of symptoms of acute mountain sickness
Actions:
Inhibits carbonic anhydrase
Decreases aqueous humor formation in eye, intraocular pressure, hydrogen secretion by renal tubules
Pharmacokinetics:
Route: Oral
Onset: 1 h
Peak: 2–4 h
Duration: 6–12 h
Sustained-release oral Onset: 2 h Peak: 8–12 h Duration: 18–24 h
IV Onset: 1–2 min Peak: 15–18 min Duration: 4–5 h
T1/2: 5 to 6 hours; excreted unchanged in urine.
Adverse Effects:
Weakness, fatigue, rash
Anorexia, nausea, urinary frequency
Renal calculi, bone marrow suppression, weight loss
Metabolic acidosis, hypersensitivity reactions, liver impairment, hypokalemia, hyponatremia
Paresthesia, tinnitus
Spironolactone – Prototype Summary
Indications:
Primary hyperaldosteronism
Adjunctive therapy in treatment of edema associated with heart failure, nephrotic syndrome, ascites associated with cirrhosis
Treatment of hypokalemia or prevention in high-risk patients
Essential hypertension; increases survival and decreases need for hospitalization in HF with reduced ejection fraction
Actions:
Competitively blocks effects of aldosterone in renal tubule
Causes loss of sodium and water; retention of potassium
Pharmacokinetics:
Route: Oral
Onset: Unknown
Peak in Plasma: 2.5–4 h
Duration: 48–72 h
T1/2: 1.4 hours for drug; about 15 hours for active metabolites; metabolized in liver and excreted in urine.
Adverse Effects:
Dizziness, headache, drowsiness
Rash, cramping, diarrhea, hyperkalemia
Hirsutism, gynecomastia, deepening of voice, irregular menses
Mannitol – Prototype Summary
Indications:
Prevention and treatment of oliguric phase of renal failure
Reduction of intracranial pressure and treatment of cerebral edema
Reduction of elevated intraocular pressure; promotion of urinary excretion of toxic substances
Diagnostic use for measurement of glomerular filtration rate; irrigant in transurethral prostatic resection and other procedures
Actions:
Elevates osmolarity of glomerular filtrate, leading to loss of water, sodium, and chloride
Creates osmotic gradient in eye, reducing intraocular pressure
Creates osmotic effect decreasing swelling after transurethral surgery
Pharmacokinetics:
Route: IV
Onset: 20–40 min Peak: 1 h
Duration: 6–8 h
Irrigant Onset: Rapid Peak: Rapid Duration: Short
T1/2: 15 to 100 minutes; excreted unchanged in urine.
Adverse Effects:
Dizziness, headache, hypotension
Rash, nausea, anorexia, dry mouth
Thirst, diuresis, fluid and electrolyte imbalances, hypersensitivity reactions, injection site reactions
Fosfomycin – Prototype Summary
Indications:
Treatment of women with uncomplicated urinary tract infections caused by susceptible bacteria
Actions:
Interferes with enzyme pyruvate transferase necessary for bacterial cell wall synthesis
Pharmacokinetics:
Route: Oral
Onset: Rapid
Peak: 2 h
Duration: Unknown
T1/2: 5.7 hours; excreted in urine.
Adverse Effects:
Headache, dizziness, nausea, diarrhea, vaginitis
Oxybutynin – Prototype Summary
Indications:
Relief of bladder instability associated with uninhibited neurogenic and reflex neurogenic bladder
Treatment of overactive bladder symptoms
Actions:
Directly relaxes smooth muscle in the bladder
Inhibits acetylcholine effects at muscarinic receptors
Pharmacokinetics:
Route: Oral
Onset: 30–60 min
Peak: 3–6 h
Duration: 6–10 h
Transdermal Onset: Slow Peak: 36 h Duration: 96 h
T1/2: 2 to 3 hours; metabolized in liver and excreted in urine.
Adverse Effects:
Dry mouth, nervousness, tachycardia
Nausea, vomiting, vision changes, flushing, sweating
Phenazopyridine – Prototype Summary
Indications:
Symptomatic relief of pain, urgency, burning, frequency, and discomfort from irritation of the urinary tract caused by infection, trauma, surgery, or procedures
Actions:
Direct topical analgesic effect on urinary tract mucosa
Pharmacokinetics:
Route: Oral
Onset: Rapid
Peak: Unknown
Duration: Unknown
T1/2: 7 to 11 hours; metabolized in liver and excreted in urine.
Finasteride – Prototype Summary
Indications:
Treatment of benign prostatic hyperplasia (BPH)
Prevention of male-pattern baldness in male patients only
Actions:
Inhibits 5-alpha–reductase, resulting in inhibition of testosterone conversion to DHT
Pharmacokinetics:
Route: Oral
Onset: Rapid
Peak: 8 h
Duration: Unknown
T1/2: 6 hours; metabolized in liver and excreted in urine and feces.
Adverse Effects:
Sexual dysfunction, gynecomastia, hypotension, rash
Dextromethorphan – Prototype Summary
Indications:
Control of nonproductive cough
Actions:
Depresses cough center in medulla to control cough spasms
Pharmacokinetics:
Route: Oral
Onset: 25–30 min
Peak: 2 h
Duration: 3–6 h
T1/2: 1 to 4 hours; metabolized in liver and excreted in urine.
Adverse Effects:
Dizziness, respiratory depression, dry mouth
Tetrahydrozoline – Prototype Summary
Indications:
Symptomatic relief of nasal and nasopharyngeal mucosal congestion due to the common cold, hay fever, or allergies
Actions:
Sympathomimetic; vasoconstriction leading to decreased edema and inflammation of nasal membranes
Pharmacokinetics:
Route: Topical (intranasal)
Onset: 5–10 min
Peak: 10–20 min
Duration: 2–6 h
T1/2: Unknown; not absorbed systemically.
Adverse Effects:
Local stinging and burning, rebound congestion
Anxiety, restlessness, tremors, hypertension
Pseudoephedrine – Prototype Summary
Indications:
Temporary relief of nasal congestion caused by common cold, hay fever, or allergies
Promotion of nasal or sinus drainage; relief of eustachian tube congestion
Actions:
Stimulates alpha-adrenergic receptors in nasal mucous membranes
Shrinks mucous membranes
Pharmacokinetics:
Route: Oral
Onset: 30 min
Peak: 1–2 h
Duration: 4–6 h
T1/2: 9 to 16 hours; excreted unchanged in urine.
Adverse Effects:
Anxiety, restlessness, headache
Dizziness, drowsiness, vision changes, hypertension, arrhythmias, sweating
Flunisolide – Prototype Summary
Indications:
Treatment of seasonal allergic rhinitis for patients not getting relief from other decongestants
Actions:
Anti-inflammatory action results from ability to block multiple inflammatory cytokines
Pharmacokinetics:
Route: Topical (nasal)
Onset: Immediate
Peak: Unknown
Duration: 4–8 h
T1/2: Unknown; minimal systemic absorption.
Adverse Effects:
Local burning, irritation, headache, dry mucosa, increased risk of infection
Diphenhydramine – Prototype Summary
Indications:
Symptomatic relief of perennial and seasonal rhinitis, vasomotor rhinitis, allergic conjunctivitis, urticaria, angioedema
Also used for motion sickness and sedation
Actions:
Blocks effects of histamine at H1-receptor sites
Has anticholinergic and antipruritic effects
Pharmacokinetics:
Route: Oral
Onset: 15–30 min
Peak: 1–4 h
Duration: 4–7 h
T1/2: 2.3 to 7 hours; metabolized in liver and excreted in urine.
Adverse Effects:
Drowsiness, sedation, dizziness
Drying of respiratory and GI mucous membranes, arrhythmias, urinary retention
Guaifenesin – Prototype Summary
Indications:
Symptomatic relief of respiratory conditions characterized by dry, nonproductive cough and presence of mucus in respiratory tract
Actions:
Enhances output of respiratory tract fluid by reducing adhesiveness and surface tension
Facilitates removal of viscous mucus
Pharmacokinetics:
Route: Oral
Onset: 30 min
Peak: Unknown
Duration: 4–6 h
T1/2: Unknown; metabolized and excreted in urine.
Adverse Effects:
Nausea, vomiting, headache, dizziness, rash
Acetylcysteine – Prototype Summary
Indications:
Mucolytic adjunctive therapy for abnormal, viscid, or inspissated mucus secretions in acute and chronic bronchopulmonary disorders
Antidote for acetaminophen overdose
Actions:
Splits bonds linking mucoproteins, decreasing viscosity
Protects liver cells from acetaminophen metabolites
Pharmacokinetics:
Route: Oral
Onset: 30–60 min
Peak: 1–2 h
Duration: Unknown Inhalation Onset: 1 min Peak: 5–10 min Duration: Unknown
IV Onset: Rapid Peak: End of infusion Duration: Unknown
T1/2: 5.6 hours; metabolized in liver and excreted in urine.
Adverse Effects:
Nausea, stomatitis, urticaria, bronchospasm, rhinorrhea
Theophylline – Prototype Summary
Indications:
Symptomatic relief or prevention of asthma; reversal of bronchospasm associated with COPD
Actions:
Directly relaxes bronchial smooth muscle, causing bronchodilation
Increases respiratory drive
Pharmacokinetics:
Route: Oral
Onset: 1–6 h
Peak: 4–8 h
Duration: 6–12 h
IV Onset: Immediate Peak: Unknown Duration: Unknown
T1/2: 3 to 15 hours; metabolized in liver and excreted in urine.
Adverse Effects:
Irritability, restlessness, dizziness
Palpitations, tachycardia, seizures, brain damage, hypotension, cardiac arrest, respiratory arrest
Albuterol – Prototype Summary
Indications:
Treatment or prevention of bronchospasm in acute or chronic asthma
Prevention of exercise-induced asthma
Actions:
Selectively stimulates beta-2 adrenergic receptors of smooth muscle in the lungs
Pharmacokinetics:
Route: Inhalation
Onset: Slow
Peak: 1–2 h
Duration: 6–8 h
T1/2: 2 to 3 hours; metabolized in liver and excreted in urine.
Adverse Effects:
Irritability, headache
Rebound congestion, epistaxis, local infection
Ipratropium – Prototype Summary
Indications:
Maintenance treatment of bronchospasm associated with COPD
Used as nasal spray for rhinorrhea
Actions:
Anticholinergic that blocks vagally mediated reflexes by antagonizing action of acetylcholine
Pharmacokinetics:
Route: Inhalation
Onset: 15 min
Peak: 1–2 h
Duration: 3–4 h
Nasal Onset: 15 min Peak: 1–2 h Duration: 6–8 h
T1/2: 1.6 hours; excreted unchanged in urine.
Adverse Effects:
Nervousness, dizziness
Headache, nausea, dry mouth, palpitations
Budesonide – Prototype Summary
Indications:
Prevention and treatment of asthma; treatment of chronic steroid-dependent bronchial asthma
Nasal spray for allergic rhinitis
Actions:
Decreases inflammatory response in airways
Increases airflow and facilitates respiration
Pharmacokinetics:
Route: Inhalation
Onset: Slow
Peak: 1–2 h
Duration: 6–8 h
T1/2: 2 to 3 hours; metabolized in liver and excreted in urine.
Adverse Effects:
Irritability, headache
Rebound congestion, epistaxis, local infection
Zafirlukast – Prototype Summary
Indications:
Prevention and long-term treatment of asthma in adults and children 5 years of age and older
Actions:
Blocks receptors for leukotrienes, components of slow-reacting substance of anaphylaxis
Blocking airway edema and processes of inflammation in the airway
Pharmacokinetics:
Route: Oral
Onset: Rapid
Peak: 3 h
Duration: Unknown
T1/2: 10 hours; metabolized in liver and excreted in urine and feces.
Adverse Effects:
Headache, dizziness, myalgia, fever
Pain, infection, diarrhea, abdominal pain, vomiting, elevated liver enzyme concentrations
Beractant – Prototype Summary
Indications:
Prophylaxis and treatment of infants with respiratory distress syndrome (RDS) who weigh at least 600 g
Actions:
Replaces surfactant missing in lungs of neonates with RDS
Pharmacokinetics:
Route: Intratracheal
Onset: Immediate
Peak: Hours
Duration: Unknown
T1/2: Distributed into lung tissues; not absorbed systemically.
Adverse Effects:
Cyanosis, bradycardia, apnea
Pneumothorax, pulmonary hemorrhage, sepsis, infection
Cimetidine – Prototype Summary
Indications:
Short-term treatment of active duodenal or benign gastric ulcers
Treatment of pathological hypersecretory conditions
Prophylaxis of stress-induced ulcers and upper GI bleeding
Treatment of erosive gastroesophageal reflux; relief of symptoms of heartburn and acid indigestion
Actions:
Selectively blocks H2 receptors, reducing gastric acid secretions
Pharmacokinetics:
Route: Oral
Onset: Varies
Peak: 1–1.5 h
Duration: 4–5 h
Adverse Effects:
Dizziness, confusion, headache
Cardiac arrhythmias, impotence, gynecomastia, diarrhea
Sodium Bicarbonate – Prototype Summary
Indications:
Symptomatic relief of upset stomach from hyperacidity
Treatment of metabolic acidosis and certain drug intoxications
Actions:
Neutralizes stomach acid by direct chemical reaction
Pharmacokinetics:
Route: Oral
Onset: Rapid
Peak: 30 min
Duration: 1–3 h
IV Onset: Immediate Peak: Rapid Duration: Unknown
T1/2: Unknown; excreted in urine.
Adverse Effects:
Gastric rupture, systemic alkalosis
Headache, irritability, muscle twitching, weakness, nausea, vomiting, diarrhea
Omeprazole – Prototype Summary
Indications:
Short-term treatment of active duodenal ulcers, GERD, erosive esophagitis, benign active gastric ulcers
Long-term treatment of pathological hypersecretory conditions
Actions:
Inhibits hydrogen–potassium adenosine triphosphatase enzyme system on secretory surface of gastric parietal cells
Blocks final step of acid production
Pharmacokinetics:
Route: Oral
Onset: Varies
Peak: 0.5–3.5 h
Duration: Unknown
T1/2: 0.5 to 1 hour; metabolized in liver and excreted in urine.
Adverse Effects:
Headache, dizziness, vertigo
Insomnia, rash, abdominal pain, nausea, vomiting
Diarrhea, upper respiratory tract symptoms
Sucralfate – Prototype Summary
Indications:
Short-term treatment of duodenal ulcers
Maintenance therapy to prevent recurrence
Actions:
Forms an ulcer-adherent complex at ulcer site
Protects against acid, pepsin, and bile salts
Pharmacokinetics:
Route: Oral
Onset: 30 min
Peak: Unknown
Duration: 5 h
T1/2: Unknown; not absorbed systemically, excreted in feces.
Adverse Effects:
Sleepiness, dizziness, vertigo
Rash, constipation, diarrhea, nausea, indigestion, dry mouth
Misoprostol – Prototype Summary
Indications:
Prevention of NSAID-induced gastric ulcers in high-risk patients
Treatment of duodenal ulcers; induction of labor
Actions:
Prostaglandin analogue that inhibits gastric acid secretion
Increases bicarbonate and mucus production
Pharmacokinetics:
Route: Oral
Onset: Rapid
Peak: 12–15 min
Duration: 2–4 h
T1/2: 20–40 min; metabolized in liver and excreted in urine.
Adverse Effects:
Nausea, vomiting, diarrhea, abdominal pain
Excessive bleeding or spotting, miscarriage, cramping, hypermenorrhea
Pancrelipase – Prototype Summary
Indications:
Replacement therapy in patients with deficient exocrine pancreatic secretions
Treatment of conditions such as pancreatitis, cystic fibrosis, steatorrhea
Actions:
Increases digestion of fats, proteins, and carbohydrates in GI tract
Pharmacokinetics:
Route: Oral
Onset: Unknown
Peak: Unknown
Duration: Unknown
T1/2: Not absorbed systemically.
Adverse Effects:
Nausea, abdominal cramps, diarrhea
Senna – Prototype Summary
Indications:
Relief of constipation
Evacuation of bowel before tests or surgery
Part of bowel preparation
Actions:
Direct effect on intestinal wall, causing increased movement and fluid secretion
Pharmacokinetics:
Route: Oral
Onset: 6–12 h
Peak: Unknown
Duration: Unknown
T1/2: Unknown; metabolized in liver and excreted in feces.
Adverse Effects:
Abdominal cramping, diarrhea
Nausea, weakness, cathartic dependence
Psyllium – Prototype Summary
Indications:
Short-term treatment of constipation
Prevention of straining; used in dietary fiber supplement
Actions:
Bulk-forming agent that increases mass of intestinal contents
Pharmacokinetics:
Route: Oral
Onset: 12–24 h
Peak: Unknown
Duration: Unknown
T1/2: Not absorbed systemically; excreted in feces.
Adverse Effects:
Abdominal distension, abdominal pain, gas
Magnesium Citrate – Prototype Summary
Indications:
Short-term treatment of constipation
To evacuate bowel for diagnostic procedure
Actions:
Saline laxative that increases motility by increasing fluid in the intestine
Pharmacokinetics:
Route: Oral
Onset: 30 min
Peak: Unknown
Duration: 3–6 h
T1/2: Unknown; excreted in feces and urine.
Adverse Effects:
Diarrhea, abdominal cramping, bloating, electrolyte disturbances
Docusate – Prototype Summary
Indications:
Prevention of straining during defecation
Stool softener for patients with hemorrhoids, cardiac patients
Actions:
Increases mixture of fat and water in stool, softening fecal mass
Pharmacokinetics:
Route: Oral
Onset: 12–72 h
Control and symptomatic relief of acute and chronic diarrhea; reduction of volume of discharge from ileostomies
Actions:
Inhibits peristalsis by directly affecting the muscles of intestinal wall
Pharmacokinetics:
Route: Oral
Peak: Unknown
Duration: Unknown
T1/2: Unknown; may be absorbed and excreted in bile.
Adverse Effects:
Bitter taste, throat irritation, diarrhea, abdominal cramps
Methylnaltrexone – Prototype Summary
Indications:
Treatment of opioid-induced constipation in patients with serious illness or receiving palliative care
Actions:
Blocks peripheral opioid receptors without affecting analgesia
Pharmacokinetics:
Route: Subcutaneous
Onset: Rapid
Peak: 30 min
Duration: Unknown
T1/2: 8 hours; excreted in urine and feces.
Adverse Effects:
Abdominal pain, nausea, diarrhea, flatulence, dizziness
Metoclopramide – Prototype Summary
Indications:
Relief of symptoms of gastroesophageal reflux
Prevention of nausea and vomiting associated with emetogenic cancer chemotherapy
Actions:
Stimulates movement of upper GI tract without stimulating gastric, biliary, or pancreatic secretions
Pharmacokinetics:
Route: Oral
Onset: 30–60 min
Peak: 1–2 h
Duration: 1–2 h
IV Onset: 1–3 min Peak: 1 h Duration: 1–2 h
T1/2: 5 to 6 hours; metabolized in liver and excreted in urine.
Adverse Effects:
Restlessness, drowsiness, fatigue
Extrapyramidal effects, Parkinson-like reactions, nausea, diarrhea
Loperamide – Prototype Summary
Indications:
Treatment of traveler's diarrhea and chronic diarrhea
Control of diarrhea due to inflammatory bowel disease
Actions:
Inhibits peristalsis by acting on the muscular wall, increasing viscosity and decreasing number of stools
Pharmacokinetics:
Route: Oral
Onset: Varies
Peak: 5 h
Duration: Up to 6 h
T1/2: 7 to 14 hours; metabolized in liver and excreted in feces.
Adverse Effects:
Abdominal pain, distension, discomfort
Dry mouth, nausea, constipation
Alosetron – Prototype Summary
Indications:
Treatment of severe, chronic, diarrhea-predominant irritable bowel syndrome (IBS) in women who have failed conventional therapy
Actions:
5-HT3 receptor antagonist slowing colonic transit time
Pharmacokinetics:
Route: Oral
Onset: Varies
Peak: 1–4 h
Duration: Unknown
T1/2: 1.5 hours; metabolized in liver, excreted in feces and urine.
Adverse Effects:
Constipation, ischemic colitis, abdominal discomfort
Prochlorperazine – Prototype Summary
Indications:
Control of severe nausea and vomiting
Actions:
Blocks dopamine in chemoreceptor trigger zone of brain
Pharmacokinetics:
Route: Oral
Onset: 30–40 min
Peak: 60–90 min
Duration: 3–4 h
Rectal Onset: 60 min Peak: 90–120 min Duration: 3–4 h
IM Onset: 10–20 min Peak: 30 min Duration: 3–4 h
IV Onset: Rapid Peak: Rapid Duration: 3–4 h
T1/2: 5 to 6 hours; metabolized in liver and excreted in urine.
Adverse Effects:
Drowsiness, dizziness, weakness
Tremor, hypertension, hypotension, cardiac arrhythmias
Dry mouth, nasal congestion, anorexia, pallor, sweating, urinary retention
Ondansetron – Prototype Summary
Indications:
Prevention of nausea and vomiting associated with emetogenic cancer chemotherapy, radiation therapy, and postoperative states
Actions:
Blocks specific receptor sites associated with nausea and vomiting, peripherally and in chemoreceptor trigger zone
Pharmacokinetics:
Route: Oral
Onset: Rapid
Peak: 1.7 h
Duration: Unknown
IV Onset: Rapid Peak: 15 min Duration: 2.5–3 h
T1/2: 3 to 6 hours; metabolized in liver and excreted in urine.
Adverse Effects:
Headache, dizziness, drowsiness
Myalgia, urinary retention, constipation, pain at injection site, hypotension
Aprepitant – Prototype Summary
Indications:
Prevention of acute and delayed nausea and vomiting associated with chemotherapy
Actions:
Selectively blocks human substance P/neurokinin 1 (NK1) receptors
Pharmacokinetics:
Route: Oral
Onset: Rapid
Peak: 4 h
Duration: Unknown
T1/2: 9 to 13 hours; metabolized in liver, excreted in urine and feces.
Adverse Effects:
Anorexia, fatigue, diarrhea
Dehydration, elevated liver enzymes