Title | Prototype Drug Chart |
---|---|
Course | Pharmacology For The Health Professions |
Institution | Northeastern University |
Pages | 9 |
File Size | 370.4 KB |
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Prototype Drug
Therapeutic Class
Mechanism of Action
Phenylephrine
Nasal decongestant, mydriatic drug, antihyposensitive
Alpha-adrenergic; sympathetic stimulation
Antihypertensive
Alpha-adrenergic antagonist Rapid decrease in peripheral resistance, reduces BP; treats hypertension Actions of parasympathetic stimulation; stimulates smoothmuscle contraction; treats nonobstructive urinary retention
Ch. 13
Prazosin Alpha blocker Ch. 13
Bethanechol
Nonobstructive urinary retention agent
Ch. 13 Direct-acting Parasympathomimetic
Physostigmine Ch. 13
Atropine Ch. 13
Muscarinic cholinergic Antidote for atropineinduced delirium
Black Box Warning
Topically- none Intranasal-burning of mucosa, rebound congestion Ophthalmic- narrow-angle glaucoma High dose = reflex bradycardia Tremor, anxiety, restlessness may occur due to stimulation of CNS; increase HR and BP Orthostatic hypotension; low dose and at bed time; reflex tachycardia due to decrease in BP
Reaction (death) with IV infusion; restrict IV unless necessary
Salivation, sweating, abdomen al cramping, hypotension.
N/A
Preg. Category C
N/A C
C
Contraindications
Bradycardia, asystole, restlessness, nervousness, seizures, salivation, urinary frequency, muscle twitching, respiratory paralysis
N/A
Blocks the parasympathetic actions of Ach and induces fight-or-flight response. Increased HR, bronchodilation, decreased motility of GI, mydraisis, decreased secretion of glands
Dry mouth, constipation, urinary retention, increased HR.
N/A
C
C
Food Interactions
Acute pancreatitis, heart disease, hepatitis, narrowangle glaucoma
Unknown
Safety during pregnancy and lactation is not established
Do not use saw palmetto or nettle root products
Asthma, epilepsy, or parkinsonism should not use.
Antagonized by angel’s trumpet, jimson weed, or scopalia
Asthma, epilepsy, diabetes, CVD, bradycardia. Discontinue if excessive sweating, diarrhea, or frequent urination occurs. Glaucoma (increases pressure within eye), obstructive disorders of GI tract, paralytic ileus, bladder neck obstruction, benign prostatic hyperplasia.
Ginkgo biloba
Careful use with suspected obstruction, active ulcer, or inflammatory disease.
Inhibits destruction of Ach by AchE
Indirect-acting parasympathomimetic
Antidote for anticholinesterase poisoning
Adverse Effects
Herbal supplements: aloe, buckthorn, cascara sagrada increase atropine’s effect
Prototype Drug Escitalopram Oxalate (Lexapro)
Therapeutic Class Antidepressant; anxiolytic SSRI
Ch. 14
Lorazepam (Ativan)
Sedative- hypnotic; anxiolytic; anesthetic adjunct
Ch. 14
Mechanism of Action SSRI increases availability of serotonin at postsynaptic receptor sites Anti-depressant activity without production of symptoms of sympathomimetic or anticholinergic activity Potentiating effects of GABA. One of the most potent benzos; half life of 10-20 hours
Benzodiazepine
Zolpidem Ch. 14
Phenobarbital
Sedative-hypnotic Nonbenzodiazepine
Antiseizure drug; sedative
Ch. 15 Barbiturate
Diazepam Ch. 15
Antiseizure drug
Facilitates GABAmediated CNS depression. Shortterm insomnia management Long-acting used for management of seizures; enhances action of GABA neurotransmitter; all seizure types except absence. Binds to GABA receptor, suppressing neuronal activity in limbic system; suppression of abnormal neuronal foci
Adverse Effects Dizziness, nausea, insomnia, somnolence, confusion, seizures
Drowsiness, sedation, amnesia, weakness, disorientation, ataxia, sleep disturbance, blood pressure changes, blurred vision, double vision, nausea, vomiting
Black Box Warning Increase risk of suicidal thinking and behavior in children, adolescents, and young adults with major depressive disorder and other psychiatric disorders N/A
Preg. Category C
D
Daytime sedation, confusion, amnesia, dizziness, depression, nausea, vomiting, sleep walking
N/A
May cause dependence, drowsiness, vitamin deficiencies, laryngospasms; severe respiratory depression, CNS depression, coma and death with OD
N/A
Short term use b/c dependence; when IV, muscular weakness, hypotension, tachycardia, respiratory depression.
N/A
B
D
D
Contraindications Not used with breastfeeding or within 14 days of MAOI therapy
Don’t use in patients with acute narrow-angle glaucoma, primary depressive disorders, psychosis.
Lactating women should not take this drug
Inadvisable in cases of hypersensitivity to barbiturates, preexisting CNS condition, porphyrias, respiratory disease, glaucoma Injection: avoid when in shock, coma, depressed vital signs, obstetrical pt, infants < 30 days old.
Food Interactions Caution with ST. john’s wort, causing serotonin syndrome and increase effects of drug
Caution with herbal supplements; kava, valerian, chamomile, hops may have additive effect with medication. Absorption is slowed with food, onset of action delayed.
Kava and valerian may potentiate sedation
Kava and chamomile
Prototype Drug
Therapeutic Class
Mechanism of Action
Adverse Effects
Phenytoin
Antiseizure drug; antidysrthymic
Desensitizing sodium channels in the CNS responsible for neuronal responsivity. Prevents spread of disruptive electrical charges. Effective against all except absence. Same action as phenytoin, but also effects GABA and calcium channels; absence and mixed type seizures
Dysrhythmias, bradycardia, ventricular fibrillation, hypotension, hyperglycemia, headache, confusion, slurred speech, insomnia, anemia.
Ch. 15
Valproic Acid
Antiseizure drug
Ch. 15
Ethosuximide
Antiseizure drug
Ch. 15
Imipramine Ch. 16
Sertraline Ch. 16
Antidepressant; treatment of nocturnal enuresis
Antidepressant
Absence seizures; depresses activity of neurons in motor cortex by elevating neuronal threshold
Blocks reuptake of serotonin and norephinephrine into nerve terminals; major depression use and bed wetting; effectiveness of drug may not occur for 2+ weeks Treatment of depression, OCD, anxiety. Inhibits reuptake of serotonin in the brain
Black Box Warning N/A
Preg. Category D
Sedation, drowsiness, GI upset, prolonged bleeding; visual disturbances, muscle weakness, tremor, psychomotor agitation, bone marrow suppressor, weight gain, ab cramps, rash, alopecia. Impair mental/physical abilities; psychosis or extreme mood swings, depression with suicidal intent, dizziness, headache, lethargy, fatigue, ataxia, sleep pattern disturbances, attention difficulty, hiccups. Bone marrow suppression and blood dyscrasias Sedation, drowsiness, blurred vision, dry mouth, cardiovascular symptosm, hypertension; photosensitivity and hypersensitivity to tricyclic drugs.
Result in fatal hepatic failure; life threatening pancreatitis ad teratogenic effects including spina bifida
Agitation, headache, insomnia, dizziness, somnolence, fatigue.
Increase risk of suicidal thinking and behavior.
D
N/A C
Increase risk of suicidal thoughts and behavior. Not approved in pediatric patients
C
C
Contraindications Hypersensitivity to hydantoin products should be careful; rash, seizures due to hypoglycemia, sinus bradycardia, and heart block
Food Interactions Herbal laxatives increase potassium loss; ginkgo reduces therapeutic effectiveness
Hypersensitivity; no one with liver disease, bleeding dysfunction, pancreatitis, and congenital metabolic disorder
Unknown
Hypersensitivity; do not use with liver or kidney disease
Ginkgo reduces therapeutic effects
Not used in acute recovery of MI, defects in bundlebranch conduction, glaucoma, hepatic impairment.
Evening primrose oil, ginkgo may lower seizure threshold; st john’s wort may cause serotonin syndrome Caution if taking St. Johns wort or L-tryptophan to avoid
Sertraline and MAOI use not advised.
Prototype Drug Phenelzine
Therapeutic Class Antidepressant
Ch. 16
Lithium
Mood stabilizing drug; bipolar disorder drug
Ch. 16
Methylphenidate
ADHD drug
Ch. 16
Chlorpromazine
Antipsychotic; schizophrenia drug
Ch. 17
Haloperidol Ch. 17
Antipsychotic; schizophrenia drug
Mechanism of Action
Adverse Effects
Black Box Warning Increase risk of suicidal thoughts and behaviors.
Irreversible inhibition of MOI; used if not responsive to other medications
Constipation, dry mouth, orthostatic hypotension, insomnia, nausea, loss of appetite.
Alter ionic activity of neurons containing dopamine, norepinephrine, and serotonin, by influencing release, synthesis, and reuptake. Activates reticular activating system, causing heightened alertness. Achieved by release of neurotransmitters such as norepinephrine and dopamine. Relief of positive symptoms; 7-8 weeks before improvement.
Dizziness, fatigue, short-term memory loss, increased urination, nausea, vomiting, loss of appetite, abdominal pain, diarrhea, dry mouth, muscular weakness, slight tremors.
Toxicity closely related to therapeutic serum concentrations
Nervousness, insomnia, irregular heartbeat, high BP, liver toxicity, causes dependence,
High abuse potential; long period usage may cause dependency
Strong blockage of alpha adrenergic receptors and weak blockage of cholinergic receptors; dizziness, drowsiness, orthostatic hypotension. EPS more common in women and elderly Less sedation and hypotension than chlorpromazine, but incidence of EPS is high. Older adults more likely to experience adverse effects.
Elderly patients with dementiarelated psychosis are at risk for death
Management of acute/chornic psychotic disorders; treat tourettes syndrome, has longacting IM or subcutaneous
Elderly patients with dementiarelated psychosis increase risk for death
Preg. Category C
D
C
C
C
Contraindications Cardiovascular or cerebrovascular disease, hepatic or renal impairment, and pheochromocytoma should not use In debilitated patients and those with severe cardiovascular disease, dehydration, renal disease.
serotonin syndrome Food Interactions Ginseng may cause headaches, tremors, mania, hallucinations, irritability. Unknown
History of marked anxiety, agitation, psychosis, suicidal ideation, glaucoma, motor tics, or Tourette’s disease should not use.
Administration relative to meals needs individual titration
Not advised during alcohol withdrawal or in coma; during lactation
Kava and st. john’s worts increase risk for dystonia
Pharmacotherapy with nonphenothiazines not advised if on meds for: parinson’s seizure disorder, alcoholism, mental
Kava may increase effects
Prototype Drug Risperidone Ch. 17
Morphine
Therapeutic Class
Treats bipolar mania/schizophrenia; treats symptoms of irritability in those with autism
EPS, hyperactivity, fatigue, nausea, dizziness, visual disturbances, fever, orthostatic hypotension.
Opioid analgesic
Binds with mu and kappa receptors; causes euphoria, constriction of pupils, and stimulation of cardiac muscles.
Restlessness, depression, anxiety, hallucinations, nausea, constipation, dizziness, itching sensation, respiratory depression and cardiac arrest in OD. Tolerance and cross-tolerance may develop.
Treatment of acute opioid overdose and misuse
Pure opioid antagonist; blocking both mu and kappa receptors; useful in OD. Reverses CNS and respiratory depression within minutes.
Minimal toxicity; reversal of effects of opioids results in rapid loss of analgesia, increased BP, tremors, hyperventilation, nausea and vomiting, and drowsiness.
Nonopioid analgesic; NSAID
Inhibits prostaglandin synthesis; limited effects on peripheral blood vessels, causing vasodilation and sweating.
GI bleeding, enteric-coated tablets and buffered preparations are available for this adverse effect.
Ch. 18
Aspirin Ch. 18
Adverse Effects
Second-generation antipsychotic; schizophrenia drug
Ch. 18
Naloxone (narcan)
administration Mechanism of Action
Black Box Warning Elderly patients with dementiarelated psychosis increase risk of death
As epidural, must be observed for 24 hours; extendedrelease tablets has abuse liability; alcohol should be avoided. None; hepatic injury when taken in excess.
Preg. Category C
B D in long term use or high dose
B
N/A D
depression. Contraindications Increased risk for heart failure, pneumonia or sudden death in elderly; underlying cardiovascular disease prone to dysrhythmias and hypotension Intensify or mask pain of gallbladder disease. Avoid in cases of severe asthma, GI obstruction, and severe hepatic or renal impairment.
Food Interactions Caution with herbal supplements such as Kava, valerian, or chamomile, increasing CNS depressive effects Yohimbe, kava kava, valerian, and st. johns wort may potentiate effect of morphine.
Not be used for respiratory depression caused by nonopioid meds.
Echinacea may increase risk of hepatotoxicity.
Not given to patients receiving other anticoagulant therapies
Feverfew, garlic, ginger, ginkgo increases risk of bleeding.
Prototype Drug
Therapeutic Class
Mechanism of Action
Adverse Effects
Sumatriptan
Antimigraine drug
Triptan group; causes vasoconstriction of cranial artiers; terminates migraines in 10-20 minutes.
Dizziness, drowsiness, warming sensation.
Blocks neuronal pain impulses; injected as nerve block for spinal and epidural anesthesia. Blocks sodium channels in membranes of neurons.
CNS excitement, irritability, confusion if OD. Convulsions, respiratory depression, cardiac arrest.
N/A
High doses, anxiety, excitement, combativeness. As it is exhaled at the end of the procedure, may have difficulty breathing. Nausea and vomiting most common with this anesthetic. Potential for abuse.
N/A
Ch. 18
Lidocaine Ch. 19
Anesthetic (local/topical); antidysrthymic
Black Box Warning N/A
Preg. Category C
B
Given IV, IM, local, or subcutaneous
Nitrous Oxide Ch. 19
General anesthetic
Suppression of pain mechanisms in the CNS; low potency and does not produce complete loss of consciousness or profound relaxation of skeletal muscles. Commonly combined as adjunct, not alone a surgical anesthetic.
N/A
Contraindications Cautiously in patients with recent MI or history of angina pectoris, hypertension, diabetes.
Avoided in sensitivity to amidtype local anesthetics. Application or injection contraindicated in presence of severe trauma or sepsis, blood dyscranias, dysrhythmias, sinus bradycardia, heart block. Impaired level of consciousness, head injury, in ability to comply with instructions, decompression sickness, undiagnosed abdominal pain, bowel obstruction, COPD, hypotension, cyanosis, chest trauma.
Food Interactions Ginkgo, ginseng, Echinacea, and st. jonh’s wort may increase toxicity.
Unkown
Milk thistle taken before or after may lower potential of liver damage; ginger may provide therapeutic benefit.
Prototype Drug Isoflurane
Therapeutic Class
Mechanism of Action
Adverse Effects
Black Box Warning
Inhaled general anesthetic
Produced potent level of anesthetic that is rapid in onset and provides smooth induction with low degree of metabolism. Muscle relaxation and used as adjunct. Cardiac output well maintained. Induction and maintenance of general anesthesia; immediate onset of action. Conscious sedation. Prevents nausea and vomiting.
Mild nausea, vomiting, tremors. Dose-dependent respiratory depression and reduction in BP; hyperthermia with elevated temperature.
N/A
Pain at injection site, apnea, respiratory depression, hypotension. Associated with metabolic abnormalities and organ system failures propofol infusion syndrome (PIF).
N/A
Skeletal muscle paralytic drug neuromuscular blocker
Acts on cholinergic receptor sites. Depolarization occurs and muscles contract. After repeated contractions, membrane is unable to repolarize. Muscle weakness and spasms. Paralysis occurs.
Cardiac arrest reported from children with undiagnosed skeletal muscle myopathy or Duchenne’s muscular dystrophy.
Antiparkinson drug
Restores dopamine in extrapyramidal areas of the brain. Combined with two other drugs, carbidopa and entacapone, preventing its enzymatic breakdown. Several months to achieve therapetic affects must cross
Can cause complete paralysis of diaphragm and intercostal muscles. Mechanical ventilation necessary. Bradycardia and respiratory depression expected. Ganglia affected in high doses, causing tachycardia, hypotension, urinary retention. High fever and muscle rigidity in genetic defects; Uncontrolled and purposeless movements, involuntary movements, loss of appetite, nausea, vomiting. Muscle twitching and spasmodic winking early signs of toxicity. Orthostatic hypotension in some patients.
Ch. 19
Propofol
General anesthetic
Ch. 19
Succinylcholine Ch. 19
Levodopa Ch. 20
Preg. Category C
B
C
N/A C
Contraindications
Food Interactions
Genetic predisposition to hyperthermia should not use. Caution with head trauma, brain neoplasms due to increase in intracranial pressure. Hypersensitivity rxn to medications containing soybean and egg. Caution with respiratory or cardiac impairment.
St. John’s wort should be discontinued 2-3 weeks prior to administration.
Caution in those with burns, trauma, neuromuscular disease, glaucoma.
Unknown
In narrow-angle glaucoma, suspicious pigmented lesions or history of melanoma, acute psychoses and severe psychoneurosis.
Kava
Unknown
Prototype Drug
Therapeutic Class
Benztropine
Antiparkinson drug