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Reteplase, Streptokinase, Tenecteplase, Urokinase
- Classification- Therapeutic: thrombolytics
- Pharmacologic: Plasminogen activators
- Acute management of
- coronary thrombosis (MI). Streptokinase and urokinase are used in the
- management of massive pulmonary emboli, deep vein thrombosis, and arterial
- thromboembolism. Alteplase is used in the management of acute ischemic stroke.
Action- Convert plasminogen to plasmin, which is then able to degreade fibrin present in clots. Alteplase, reteplase, tenecteplase, and urokinase directly activate plasminogen. Strepokinase combinews in plasminogen to form activator complees, which then convert plasminogen to plasmin. Therapeutic: Lysis of thrombi in coronary arteries, with preservation of ventricular function or improvement of ventricular function, decrease risk of CHF or death.
Contraindications/precautions- contraindicated in active internal bleeding; history of cerebrovascular accident; recent (within 2 mos) intracranial or intraspinal injury or trauma; intracranial neoplasm, AV malformation or aneurysm; severe uncontrolled hypertension; known bleeding tendencies; hypersensitivity; cross sensitivity with other thrombolytics may occur.
Life threatening adverse reactions/most common side effects- CNS: intracranial hemorrhage, EENT: epistaxis, gingival bleeding. RESP: bronchospasm hemoptysis, CV: hypotension, reperfusion arrhythmias, GI: GI bleeding, retroperitoneal bleeding, nausea, vomiting, GU: GU tract bleeding, DERM: ecchymoses, flushing, urticaria HEMAT: bleeding LOCAL: hemorrhage at injection sites, phlebitis at IV site. MS: musculoskeletal pain MISC: allergic reactions including anaphylaxis fever.
- Classification- Therapeutics: Vascular headache suppressant
- Pharmacologic: Ergot alkaloids
- Treatment of vascular headaches including:
- Migraine with or without
- aura, Cluster
Action- Vasoconstriction of dilated blood vessels by stimulating alpha adrenergic and serotonergic (5-HT) receptors. Larger doses may produce alpha-adrenergic blockade and vasodilation. Therapeutic: constriction of dilated carotid artery bed with resolution of vascular headache.
Contraindications/precautions- Contraindicated in peripheral vascular disease; ischemic heart disease; uncontrolled hypertension; severe renal or liver disease; malnutrition; known alcohol intolerance. Use cautiously in illnesses associated with peripheral vascualr pathology such as diabetes mellitus. Concurrent administration of other vasoconstrictor agents. PEDI: safety not established
Life threatening adverse reactions/most common side effects- CNS: dizziness, EENT: rhinitis (NASAL), CV: MI, hypertension, angina pectoris, arterial spasm, intermittent claudication, GI: abdominal pain, nausea, vomiting, altered tase (nasal) diarrhea, polydipsia MS: extremity stiffness, muscle pain, stiff neck, stiff shoulders, neuro: leg weakness, numbness or tingling in fingers or toes. MISC: fatigue
- Classification- Therapeutic: antiparkinson agents
- Pharmacologic: dopamine agonists
- Indications- Parkinson's disease
- Not useful for
- drug-induced extrapyramidal reactions
Action- Levodopa is converted to dopamine in the CNS; where it serves as a neurotransmitter. Carbidopa, a decarboxylase inhibitor, prevents peripheral destruction of levodopa. Therapeutic: relief of tremor and rigidity in parkinson's syndrome.
Contraindications/precautions- hypersensitivity, angle closure glaucoma; MAO inhibitor therapy; malignant melanoma; undiagnoses skin lesions; some products contain tartrazine, phenylanine, or aspartame and should be avoided in patients known with hypersensitivity. Us cautiously in: history of cardiac, psychiatric, or ulcer disease; OB, Pedi: safety not established; lactation: may decrease serum prolaction.
Life threatening adverse reactions/most common side effects- CNS: involuntary movements, anxiety, anxiety, dizziness, hallucinations, memoery loss, psychiatric problems, urges (gambling, sexual). EENT: blurred vision, mydiraisis. GI: nausea, vomiting, anorexia, dry mouth, hepatotoxicity. Derm: melanoma, Hemat: hemolytic anemia, leukopenia, MISC: darkening of urine or sweat.
- Classification- Therapeutic: antiparkinson's agent
- Pharmacologic: catchol-o-methyltransferase inhibitors
- With levodopa/carbidopa to
- treat idiopathic Parkinson's disease when signs and symptoms of end-of-dose
- "wearing-off" (so-called fluctuating patients) occur.
Action- Acts as a selective and reversible inhibitor of the enzyme catechol o methyltransferase (COMT). Inhibition of the enzyme prevents the breakdown of levodopa, increasing availability to the CNS. Therapeutic: prolongs duration of response to levodopa with end of dose motor fluctuations. Decreased signs and symptoms of parkinsons disease.
Contraindications/precautions- Hypersensitivity; concurrent nonselective MAO inhibitor therapy. Use cautiously in: hepatic impariment; concurrent use of durgs that are metabolized by COMT; OB, lactation: safety not established in children.
Life threatening adverse reactions/most common side effects- CNS: neuroleptic malignant syndrome, dizziness, hallucinations, syncope, urges (gambling, sexual) RESP: pulmonary infiltrates, pleural effusion, pleural thickening, CV: hypotension, DERM: melanoma, GI: abdominal pain, diarrhea, nausea, retroperitoneal fibrosis, GU: brownish-orange discoloration urine. MS: rhabdomyolysis NEURO: dyskinesia
- Classification- Therapeutic: antineoplastics, immune modifiers
- Pharmacologic: antitumor antibiotics
- Acute nonlymphocytic
- leukemia (ANLL) in adults (with other antineoplastics).
- Initial chemotherapy for
- patients with pain associated with advanced hormone-refractory prostate cancer.
- Secondary (chronic)
- progressive, progressive relapsing, or worsening relapsing-remitting multiple
- sclerosis (MS).
- Unlabelled Use(s):
- Breast cancer, liver cancer, and non-Hodgkin's
Action- Inhibits DNA synthesis (cell cycle phase- nonspecific) Therapeutic: death of rapidly replicating cells, particularly malignant ones. Decreased pain in patients with advanced prostate cancer. Decreased disability and slowed progession of MS.
Contraindications/precautions- Hypersensitivity; pregnancy or lactation. Use cautiously in previous cardiac disease; OB: patients with childbearing potential; active infection, decrease bone marrow reserve; previous mediastinal radiation; imparied hepatobiliary function; PEDI: safety not established GERI: may have increased sensitivity to drug effects
Life threatening adverse reactions/most common side effects- CNS: seizures, headache. EENT: blue-green sclera, conjuctivitis. RESP: cough, dypnea CV: Cardiotoxicity, arrhythmias, ECG changes GI:abdominal pain, diarrhea, hepatoxicity, nausea, vomiting GU: blue green urine, gonadal suppression, renal failure. DERM: alopecia, rashes, HEMAT: anmeia, leukopenia, soecndary leukemia, thrombocytopenia METAB: hyperuricemia. MISC: fever, hypersensitivity reactions.
Classification- Therapeutic: antispasticity agents, skeletal muscle relaxants (centrally acting)
Indications- Treatment of reversible spasticity due to multiple sclerosis or spinal cord lesions IT: treatment of severe spaticity origniating in the spinal cord. Unlabeled: management of pain in trigeminal neuralgia
Action- Inhibits reflexes at the spinal level. Therapuetic: decrease muscle spasticity; bowel and bladder function may also be improved.
Contraindications/precautions- Contraindicated in hypersensitivity; orally disinegrating tablets contain aspartame and should not be used in patients with pheylketonuria. Use catuiously in: patients in whom spasticity maintains posture and balance; patients with epilepsy may decrease seizure threshold GERI: increase risk of CNS side effects.
Life threatening adverse reactions/most common side effects- CNS: seizures, dizziness, dorwsiness, fatigue, weakness, confusion, depression, headache, insomnia, EENT: nasal congestion, tinnitus, CV: edema, hypotension GI: nausea, constipation. GU: frequency DERM: pruritus, rash, METAB: hypreglycemia, weight gain NEURO: ataxia MISC: hypersensitivity reactions, sweating.
- Classification- Therapeutic: antimyasthenics
- Pharmacologic: cholinergic
Indication- Used to increase muscle strength in symptomatic treatment of myasthenia gravis. Reversal of nondepolarizing neuromuscular blocking agents. Prophylaxis of lethal effects of poisoning with the nerve agent soman.
Action- Inhibits the breakdown of acetlycholine and prolongs its effects (anticholinesterase). Effects include: miosis, increased intestinal and skeletal muscle tone, bronchial and ureteral constriction, bradycardia, increased slaivation, lacrimation, sweating. Therapeutic: improved musclular function in patients with myasthenia gravis. Reversal of paralysis from nondepolarizing nueromuscular blocking agents. Prevention of soman nerve gas toxicity.
Contraindications/precautions- contraindicated in hypersensitivty to pyridostigmine or bromides; mechanical obstruction of the GI or GU tract; known alcohol intolerance (syrup only) use cautiously in history of asthma; ulcer disease; cardiovascular disease, epilepsy, hyperthyroidism, OB: may cause uterine irritability after IV admin. near term; 20% of newborns display transient muscle weakness, lactation: pedi: safety not established.
Life threatening adverse reactions/most common side effects- Drug-drug- cholinergic effects may be antagonized by other drugs possessing anticholinergic properties, including antihistamines, antidepressants, atropine, haloperidol, phenothiazines, procainamide, quininine, or disopyramide. Prolongs the action of depolarizing muscle relaxing agents and cholinesterase inhibitors (succinlycholine decamethonium) increases toxicity with other cholinesterase inhibitors, including echothiophate.
- Classification- Therapeutic: antiplatelet agents
- Pharmacologic: platelet aggregation inhibitors
Indication- Prevention of stroke in patients who have had a completed thromolytic stroke or precursors to stroke and are unable to tolearte aspirin. Unlabeled use: prevention of subacute stent thrombosis in patients receiving intracoronary stents (given with aspirin)
Action- Inhibits platelet aggregation by altering the function of platelet membranes. Prlongs bleeding time. Therapeutic: decreased incidence of stroke in high risk patients. Decreased incidence of subacute stent thrombosis.
Contraindications/precautions- hypersensitivity, bleeding, disorders, active bleeding, severe liver disease, use cautiously in risk for bleeding (trauma, surgery, history of ulcer disease); renal or hepatic impairment PEDI, OB, safety not established GERI: appears on beers list. increased sensitivity
Life threatening adverse reactions/most common side effects- CNS: dizziness, headache, weakness EENT: epistaxis, tinnitus GI: diarrhea, abnormal liver function tests, anorexia, gi fullness, gi pain, neause, vomitig, GU: hematuria, DERM: rashes, ecchymoses, pruritus, urticaria, HEMAT: agranulocytosis, aplastic anemia, intracerberal bleeding, neutropenia, bleeding thrombocytopenia. Metab: hyperchoesterolemia, hypertriglyceridemia.
- Classification- Therapeutic: Vascular headache suppresants
- Pharmacologic: 5-HT, agonists
Indications- Acute treatment of migraine attacks. Subcut: Acute treatment of cluster headache episodes.
Action- Acts as a selective agonist of 5 HT, at specific vascular serotonin receptor sites, causing vascoconstriction in large intracranial arteries. Therapeutic: relief of acute attacks of migraine.
Contraindications/precautions- Hypersensitivity; patients with ischemic heart disease or signs and symptoms of ischemic heart disease, prinzmetal angina or uncontrolled hypertension; stroke or transient ischemic heart disease, ischemic heart attack. ischemic bowel disease, concurrent MAO inhibitor therapy GERI: excessive risk of cardiovascular complications.
- Life threatening adverse reactions/most common side effects- Less common after oral administration.
- CNS: dizziness, vertigo, anxiety, drowsiness, fatigue, feeling of heaviness, feeling of tightness, headache, malaise, strange feeling, tight feeling in head, weakness, EENT: alterations in vision, nasal sinus discomfort, throat discomfort, CV: MI angina, chest pressure, chest tightness, coronary vasospasm, ECG changes, transient hypertension GI: abdominal discomfort, dysphagia, DERM: tingling, warm sensation, burning sensation, cool sensation, flushing LOCAL: injection site reaction MS: jaw discomfort, muscle cramps, myalgia, neck pain, neck stiffness.
- Classification- Therapeutic: antiparkinson agents
- Pharmacologic: monoamine oxidase type B inhibitors
Indications- Management of parkinon's disease (with levodopa or levodopa/carbidopa) in patients who fail to respond to levodopa/carbidopa alone.
Action- Following conversion by MAO to it's active form, selegiline inactivates MAO by irreversibly binding to it at type B (brain sites). Inactivation of MAO leads to increased amounts od dopamine available in the CNS. Therapeutic: increased response to levodopa/dopamine therapy in Parkinson's disease.
Contraindications/precautions- Hypersensitivity; concurrent meperidine or opioid analgesic therapy (possible fatal reactions); concurrent use of SSRI's or tricyclic antidepressants. Use cautiously in doses >10 mg/day increase risk of hypersensitive reactions with tyramine containing foods and some medications) history of peptic ulcer disease
Life threatening adverse reactions/most common side effects- CNS: confusion, dizziness, fainting, hallucinations, insomnia, urges (gambling, sexual), vivid dreams DERM: melanoma GI: nausea, abdominal pain, dry mouth
Classification- Therapeutic: anticonvulants, mod stabilizers
Indications- Treatment of tonic clonic, mixed, and complex partial seizurs. Management of pain in trigeminal neuralgia or diabetic neuropathy. Equetro only: Acute mania and mixed mania. Unlabeled use: other forms of neurogenic pain.
Action- Decreases synaptic transmission in the CNS by affecting sodium channels in neurons. Therapeutic: prevention of seizures. Relief of pain in trigeminal neuralgia, decreased mania.
- Contraindications/precautions- Hypersensitivity; bone marrow suppression; concomitant use or use within 14 days of MAO inhibitors; OB: use only during pregnancy if potential benefits outweigh risks to the fetus; additional vitamin K during last weeks of pregnancy has been recommended. Lactation: discontinue drug or bottle feed.
- Use cautiously in: all patients, may increase risk of suicidal thoughts, cardiac or hepatic disease; renal failure, increase intraocular pressure. GERI: older men with hyperplasia may be at risk for increased acute urinary retention or difficulty initiating steam. EXTREME CAUTION: patients positive for HLA_B 1502 allele unless benefits outweigh risk.
Life threatening adverse reactions/most common side effects- CNS:suicidal thoughts, ataxia, drowsiness, fatigue, psychosis, sedation, vertigo EENT: blurred vision, nystagmus, corneal opacities, RESP: pneumonitis CV: CHF, edema, hypertension, hypotension, syncope, GI: hepatitis, pancreatitis, weight gain GU: hesistancy, urniary retention DERM: photosensitivity, rashes, STEVEN JOHNSON SYNDROME, TOXIC EPIDERMAL NECROLYSIS, urticaria. ENDO: syndrome inappropriate antidiuretic hormone, hyponatremia, HEMAT: agranulocytosis, aplastic anemia, thrombocytopenia, eosinophilia, leukopenia, MISC: chills, fever, ymphadenopathy, increased liver enzymes, multi organ hypersensitivity reactions, hepatic failure (rare).
Classification- Therapeutic: skeletal muscle relaxants (centrally acting)
Indications- Management of acute painful musculoskeletal conditions associated with muscle spasm. Unlabeled: management of fibromyalgia.
Action- Reduces tonic somatic muscle activity at the level of the brainstem. Structurally similar to tricyclic antidepressants. Therapeutic: reduction in muscle spasm and hyperactivity w/o loss of function.
Contraindications/precautions- Hypersensitivity; should not be used w/in 14 days of MAO inhibitor therapy; immediate period after MI; severe or symptomatic cardiovascular disease, cardiac conduction disturbances, hyperthyroidism. Use cautiously in: cardiovascular disease; GERI: appears on Beers list. Poorly tolearted due to anticholinergic effects; OB, Lactation, Pedi: pregnancy, lactation and children <15yr (safety not established).
Life threatening adverse reactions/most common side effects- CNS: dizziness, drowsiness, confusion, fatigue, headache, nervousness, EENT: dry mouth, blurred vision, CV: arrhythmias, GI: constipation, dyspepsia, nausea, unpleasant taste GU: urinary retention
Classification- Therapeutic: acetylcholinestrase inhibitor
Indications- used to differentiate myasthenia gravis from cholinergic crisis andLambert-Eaton myasthenic syndrome.
Action- In myasthenia gravis, the body produces autoantibodies which block, inhibit or destroy Nicotinic acetylcholine receptors in the neuromuscular junction. Edrophonium - an effectiveacetylcholinesterase inhibitor - will reduce the muscle weakness by blocking the enzymatic effect ofacetylcholinesterase enzymes, prolonging the presence of acetylcholine in the synaptic cleft. In a cholinergic crisis, where a person has too much neuromuscular stimulation, edrophonium will make the muscle weakness worse by inducing a depolarizing block
Contraindications/precautions- Abnormal Heart Rhythm, Asthma, Stomach or Intestine Blockage, Urinary Tract Blockage
Life threatening adverse reactions/most common side effects- Slow heart rate, chest pain, weak pulse, shallow swallowing, urinating more than usual, seizures, watery eyes, weakness, muscle twitching.
- Classification- Therapeutic: antiplatelet agents, diagnostic agents
- Pharmacologic: platelet adhesion inhibitors
Indications- PO: prevention of thromboembolism in patients with prosthetic heart valves (with warfarin). Maintains patency after surgical grafting procedures, including coronary artery bypass (with aspirin) IV: as an alternative to exercise in myocardial perfusion scintigraphy (cardiac stress testing with radiotracer imaging)
Action- PO: decreases platelet aggregation by inhibiting the enzyme phosphodiesterase IV: produces coronary vasodilation by inhibiting adensoine uptake. Therapeutic: PO: inhibition of platelet aggregation and subsequent thromboembolic events. IV: in diagnostic thallium imaging, dipyridamole dilates normal coronary arteries, reucing flow to vessels that are narrowed and causing abnormal thallium distribution.
- Contraindications/precautions- hypersensitivity, hypotensive patients GERI: appears on Beers list, geriatric patients may be more susceptible to orthostatic hypotension; patients with platelet defects; pregnancy safety not established.
- Life threatening adverse reactions/most common side effects-
- Classification- Therapeutic: vascular headache suppressants
- Pharmacologic: 5 HT, agonists
Indications- Acute treatment of migraine headache
Action- Acts as an agonist at specific 5 HT, receptor sites in intracranial blood vessels and sensory trigeminal nerves. Therapeutic: cranial vessel vasoconstriction with associated dcrease in release of neuropeptides and resultant decrease in migraine headache.
Contraindications/precautions- Hypersensitivity, ischemic or vasospastic cardiovascular, cerebrovascular, or peripheral vascular syndromes; history of significant cardiovascular disease; uncontrolled hypertension; should not be used w/in 24hr of other 5-HT, agonists, or ergot-type compounts; basilar or hemiplegic migrain; concurrent MAO inhibitor therapy, phenylketonuria, use cautiously in: severe renal impairment, especially in patients with dialysis; moderate hepatic impairment; OB, PEDI: safety not established. EXTREME CAUTION: cardiovascular risk factors, hypertension, hypercholestrolemia, cigarette smoking, obesity, diabetes, strong family history
Life threatening adverse reactions/most common side effects- CNS: dizziness, drowsiness, weakness, CV: coronary artery vasospasm, MI, ventricular arrhytmias, ches pain, myocardial ischemia, GI, dry mouth, nausea, MISC: hypersensitivity reactions including angioedema, toxic epidermal necrolysis, pain.
- Classification- Therapeutic: antiparkinson agents
- Pharmacologic: dopamine agonists
Indications- Management of Parkinson's disease. Restless syndrome.
Action- Stimulates dopamine receptors in the striatum of the brain. Therapeutic: decreased tremor and rigidity in Parkison's disease. Decreased leg restlessness.
Contraindications/precautions- Hypersensitivity. Use cautiously in renal impairment, increased dosing interval recommended if CCr <60 mL/min PED: safety not established.
Life threatening adverse reactions/most common side effects- CNS: sleep attacks, amnesia, dizziness, drowsiness, hallucinations, weakness, abnormal dreams, confusion, dyskinesia, extrapyramidal syndrome, headache, insomnia, urges, CV: postural hypotension DERM: melanoma GI: consitpation, dry mouth, dyspepsia, nause, tooth disease, GU: urinary frequency MS: leg cramps Neuro: hypertonia, unsteadiness/falling
- Classification- Therapeutic: anti-multiple sclerosis agents, immune modifiers
- Pharmacologic: interferons
Indications- Relapsing forms of multiple sclerosis
Action- Antiviral and immunoregulatory properties produced by interacting with specific receptor sites on cell surfaces may explain beneficial effects produced by recombinant DNA technology. Therapeutic: reduce incidence of relapse (neurologic dysfunction) and slow physical disability.
Contraindications/precautions- Hypersensitivity to natural or recombinant interferon beta or human albumin. Use cautiously in history of suicde attempt or depression; history of seizures, cardiovascular disease, liver disease, history of alcohol abuse, patients with childbearing potential OB: may increase risk of spontaneous abortion; use only if potential maternal benefit outweighs potential fetal risk LACTATION: safety not established PEDI: safety not established.
Life threatening adverse reactions/most common side effects- CNS: seizures increasaed with interferon beta-1A, depression, dizziness, fatigue, headache, insomnia, drowsiness, incoordination, rigors, suicidal ideation EENT: sinusitis, vision abnormalities. RESP: dyspnea, upper respiratory tract infection. CV: chest pain, edema, hypertension GI: constipation, nausea, vomiting, abdominal pain, auto immune hepatitis, dry mouth, elevated liver function tests GU: cystitis, erectile dysfunction, polyuria, urinary incontinence. Derm: rashes, alopecia, EDNO: menstrual disorders, hyperthyroidism, hypothyroidism, menorrhagia, spontaneous abortion HEMAT: neutropenia, anemia, eosinophilia, thrombocytopenia LOCAL: injection site reactions, injection site necrosis MS: myalgia, arthralgia, muscle spasm MISC: allergic reactions including ANAPHYLAXIS, chills, fever, flue like symptoms, pain.
Classification- Therapeutic: analgesic adjuncts, therapeutic, anticonvulsants, mood stabilizers
Indications- Partial seizures (adjunct reatment) post hepetic neuralgia. Unlabeled use: neuropathic pain. Prevention of migraine headache. Bipolar disorder. anxiety. Diabetic peripheral neuropathy.
Action- Mechanism of action is not know. May affect transport of amino acids across and stabilize neuronal membranes. Therapeutic: decreased incidence of seizures. Decreased post herpetic pain.
Contraindications/precautions- Hypersensitivity. Use cautiously in all patients may increase risk of suicidal thoughts or behaviors) renal insufficiency decrease dose and/or increase dosing interval OB/PEDI: safety not established GERI: may be more susceptible to toxicity due to age related decrease in renal function.
Life threatening adverse reactions/most common side effects- CNS: sucidial thoughts, confusion, depression, drowsiness, sedation, anxiety, concentration difficulties (children), hostility, hyperkinesia (children), malaise, vertigo, weakness EENT: abnormal vision, nystagmus CV: hypertension GI: weight gain, anorexia, flatulence, gingivitis MS: arthralgia NEURO: ataxia, altered reflexes, hyperkinesia, paresthesia MISC: facial edema
- Classification- Therapeutic: antimyasthenics
- Pharmacologic: cholinergics
Indications- Improvement in muscle strength in symptomatic treatment of myasthenia gravis. Prevention and treatment of postoperative bladder distention and urinary retention or ileus. Reversal of nondepolarizing neuromuscular blockers.
Action- Inhibits the breakdown of acetylcholine so that it accumulates and has a prolonged effect. Effects inclue miosis, increased intestinal and skeletal muscle tone, bronchial and uteral constriction, bradycardia, increased salivation, lacrimation and sweating. Therapeutic: improved muscular function in patients with myasthenia gravis, improved bladder empyting in patients with urinary retention, or reversal of nondepolarizing neuromuscular blockers.
Contraindications/precautions- Hypersensitivity, mechanical obstruction of GI or GU tract; use cautiously in history of asthma; ulcer disease; cardiovascular disease, epilepsy, hyperthyroidism, OB: may cause uterine irritability after IV admin near term, newborns muscle weakness.
Life threatening adverse reactions/most common side effects- CNS: seizures, dizziness, weakness, EENT: lacrimation, miosis RESP: bronchospasm, excess secretions CV: bradycardia, hypotension GI: abdominal cramps, diarrhea, excess salivation, mausea, vomiting DERM: sweating, rash.