Adrenegic Agents

(Sympathomimetics)

Prototype drug: phenylephrine (Neo-Synephrine

Primary use: depends on receptors activated

-Alpha 1 receptors: nasal congestion, hypotension, dilation of pupils for eye exam

-Alpha 2 receptors: hypertension

-Beta 1 receptors: cardiac arrest, heart failure, shock

-Beta 2 receptors: asthma and premature-labor contractions

Adverse effects: tachycardia, hypertension, dysrhythmias, CNS excitation and seizures, dry mouth, nausea and vomiting, anorexia

Prototype drug: prazosin (Minipress)

Mechanism of action: blocks input to target organs from the sympathetic nervous system

Primary use: hypertension, dysrhythmias, angina, heart failure, benign prostatic hypertrophy, narrow-angle glaucoma

Adverse effects: dizziness, drowsiness, headache, loss of energy and strength, palpitations, dry mouth

Cholinergic Agents

(Parasympathomimetics)

Prototype drug: bethanechol ( Urecholine)

Mechanism of action: activates target organs of the parasympathetic nervous system directly/indirectly

-Direct action: muscarinic agonists

-Indirect action: acetylcholinesterase inhibitors, also activate nicotinic receptors because of more acetylcholine

Primary use: glaucoma, urinary retention, myasthenia gravis, Alzheimer's disease

Adverse effects: profuse salication, increased muscle tone, urinary frequency, bronchoconstriction, bradycardia

Prototype drug: atropine (Atropair, Atropisol)

Mechanism of action: blocks input to target organs of the parasympathetic nervous system

Primary use: peptic ulcers, irritable bowel syndrome, mydriasis (pupil dilation) and cycloplegia (loss of accomodation) during eye exam, bradycardia, preanesthetic, asthma

Adverse effects: tachycardia, CNS stimulation, urinary retention, dry mouth, dry eyes, decreased sweating, photophobia

Prototype drug: lorazepam (Ativan)

Mechanism of action: binds to GABA receptor-chloride channel molecule, which intensifies GABA effects

Primary use: for anxiety disorders and insomnia

Adverse effects: drowsiness, dizziness, respiratory depression

Prototype drug: phenobarbital (Luminal)

Mechanism of action:

-binds with GABA receptor-chloride channel molecules, intensifying effects of GABA

-inhibits brain impulses from passing through limbic and reticular activating systems

Primary use: as sedative and hypnotic

Adverse effects: tolerance, respiratory depression, psychological and physical dependence

Nonbenzodiazepines, Nonbarbiturate

(CNS depressant)

Prototype drug: zolpidem (Ambien)

Mechanism of action: bings to GABA receptors

Primary use: as hypnotic (short term 7-10 days)

Adverse effects: mild nausea, dizziness, diarrhea, daytime drowsiness, amnesia

Barbiturates

(seizure)

Prototype drug: phenobarbital (Luminal)

Mechanism of action: enhancing the action of GABA

Primary use: controlling seizures

Adverse effects: dependence, drowsiness, vitamin deficiencies, laryngospasm

Benzodiazepines

(seizures)

Prototype drug: diazepam (Valium)

Mechanism of action: similar to that of barbiturates, but safer

Primary use: for short-term seizure control

Adverse effects: drowsiness and dizziness

Prototype drug: valproic acid (Depakene)

Mechanism of action: similar to that of barbiturates and benzodiazepines on GABA

Primary use: as adjunct therapy

Adverse effects: sedation, drowsiness, GI upset, prolonged bleeding time

Prototype drug: phenytoin (Dilantin)

Mechanism of action: desensitize sodium channels

Primary use: treating all types of epilepsy except absence seizures

Adverse effects: skin rash, cardiac dysrhythmias, and hypotension

Prototype drug: vaprroic acid (Depakene)

Mechanism of action: desensitize sodium channels

Primary use: for absence of seizures

Adverse effects: limited CNS depression, visual disturbances, ataxia, vertigo, headache

Additional adverse reactions: gastrointestinal effects, hepatotoxicity, pancreatitis

Prototype drug: ethosuximide (Zarontin)

Mechanism of action: suppress calcium influx

Primary use: for absence of seizures

Adverse effects: rare but include drowsiness, dizziness, lethargy

Very rare but serious side effects: systemic lupus erythematosis, leukopenia, aplastic anemia, Stevens-Johnson syndrome

Tricyclic Antidepressants

(TCAs)

Prototype drug: imipramine (Trofranil)

Mechanism of action: to inhibit reuptake of norepinephrine and serotonin

Primary use: for major depression

Adverse effects: orthostatic hypotension, sedation and anticholinergic effect, rarely, cardiac dysrhythmias

Selective Serotonin Reuptake Inhibitors

(SSRIs)

Prototype drug: sertraline (Zoloft)

Mechanism of action: to slow the reuptake of serotonin

Primary use: depression

Adverse effects: sexual dysfunction, nausea, headache, weight gain, anxiety, insomnia

Less common side effects: sedation, anticholinergic effects, sympathomimetic effects

Atypical Antidepressants: Norepinephrine & Dopamine Reuptake Inhibitors

(NDRIs)

Prototype drug: bupropion (Wellbutrin)

Mechanism of action: to inhibit reuptake of norepinephrine & dopamine

Primary use: for depression

Adverse effects: headache, insomnia, hypertension; stimulant properties (may be beneficial)

Atypical Antidepressants: Selective norepinephrine reuptake inhibitor

(SNRI)

Prototype drug: venlafaxine (Effexor)

Mechanism of action: to selectively inhibit reuptake of norepinephrine

Primary use: for depression

Adverse effects: headache, insomnia, hypertension

Prototype drug: phenelzine (Nardil)

Mechanism of action: to decrease effectiveness of monoamine oxidase; increase norepinephrine available at receptors

Primary use: for depression

Adverse effects: orthostatic hypotension, headache, insomnia, and diarrhea;

-also interact with a large number of foods and other medications

Mood Stabilizers

Prototype drug: lithium carbonate (Eskalith)

Mechanism of action: affects sodium transport across cell membranes

Primary use: bipolar disorder

Adverse effects: excessive loss of sodium, weight gain (can be extreme)

Prototype drug: methylphenidate hydrochloride (Ritalin)

Mechanism of action: blocks norepinephrine pumps (vesicular & re-uptake); heightens awareness, increases focus

Primary use: to treat attention deficit/hyperactivity disorder (ADHD)

Adverse effects: insomnia, nervousness, anorexia, weight loss

Phenothiazines:

"conventional (typical)"

Antipsychotic Agents

Prototype drug: phenothiazine/chlorpromazine (Thorazine)

Mechanism of action: reduces or eliminates positive symptoms of schizophrenia; antagonist at D2 receptors

Primary use: psychosis

Adverse effects: acute dystonia, akathisia, Parkinsonism, tardive dyskinesia, anticholinergic effects, sedation, hypotension, sexual dysfunction, and neuroleptic malignant syndrome

Nonphenothiazines:

"conventional (typical)"

Antipsychotic Agents

Prototype drug: haloperidol (Haldol)

Mechanism of action: reduces or eliminates positive symptoms of schizophrenia; antagonist at D2 receptors

Primary use: psychosis

Adverse effects: identical to that of phenothiazines

Prototype drug: clozapine (Clozaril)

Mechanism of action: block dopamine type 2 receptors, serotonin and alpha-adrenergic receptors

Primary use: psychosis; treats both positive and negative symptoms of schizophrenia

Adverse effects: fewer than those of phenothiazines and nonphenothiazines, but obesity and its risk factors need to be monitored

Prototype drug: morphine

Mechanism of action: agonist at opioid receptors

Primary use: for analgesia and anesthesia

Adverse effects: respiratory depression, sedation, nausea, and vomiting

Prototype drug: acetaminophen (Tylenol)

Mechanism of action: to treat fever; at the level of the hypothalamus and causes dilation of peripheral blood vessels enabling sweating and dissipation of heat

Primary use: treatment of fever and to relieve pain

Adverse effects: uncommon with therapeutic doses

Nonsteroidal Anti-Inflammatory Drugs

(NSAIDs)

Prototype drug: ibuprofen (Motrin)

Mechanism of action: to inhibit cyclooxygenase and prevent formation of prostaglandins

Primary use: for mild or moderate pain and to reduce inflammation

Adverse effects: GI upset, acute renal failure

Prototype drug: aspirin (ASA)

Mechanism of action: as anticoagulant, antipyretic, anti-inflammatory, and analgesic

Adverse effects: with high doses may cause GI distress and bleeding

-may increase action of oral hypoglycemic agents

Prototype drug: celecoxib (Celebrex)

Mechanism of action: is similar to the NSAIDs, but selective for Cox-2 (NSAIDs inhibit both Cox-1 and Cox-2)

Primary use: osteoarthritis

Adverse effects: increased risk of serious cardiovascular thrombotic events, myocardial infarction, and stroke, which can be fatal; mild and related to GI system

Prototype drug: tramadol (Ultram)

Mechanism of action: has weak opioid activity

Primary use: as centrally acting analgesic

Adverse effects: CNS, GI, CV and dermatologic effects

Antimigraine Agents

(Triptans)

Prototype drug: sumatriptan (Imitrex)

Mechanism of action: to act as serotonin agonists, constricting certain intracranial vessels

Primary use: to abort migraines with or without auras

Adverse effects: GI upset

Mechanism of action: to promote vasoconstriction

Primary use: to terminate ongoing migraines

Adverse effects: GI upset, weakness in the legs, myalgia, numbness and tingling in fingers and toes, angina-like pain, tachycardia

Prototype drug: lidocaine (Xylocaine)

Mechanism of action: to stop axonal conduction by blocking sodium channels

Primary use: for brief medical or dental procedures

Adverse effects uncommon:

-CNS stimulation with early adverse effects

-CNS depression with later adverse effects

-Rash; allergies to sulfites used as preservative

Prototype drug: procaine (Novocain)

Mechanism of action: to stop axonal conduction by blocking sodium channels

Primary use: for brief medical or dental procedures

-amides have largely replaced the esters

General Anesthetic: Inhalation Agents

(gases or volatile liquids)

Prototype drug: nitrous oxide

Mechanism of action: prevent flow of sodium into CNS; reduce neural activity

Primary use: with IV agents to maintain loss of consciousness; used alone for dental procedures

Adverse effects: nausea and vomiting, CNS depression, respiratory difficulty, vital-sign changes

General Anasthetic: IV

(Barbiturate and barbiturate-like agents, opioids, benzodiazepines)

Prototype drug: thiopental sodium (Penthonal)

Primary use:

-used in combo with inhalation agents (fewer side effects)

-produces unconsciousness quickly and amnesia

-some used for conscious sedation

Adverse effects: allergic reactions, dysrhythmias, respiratory depression

Prototype drug: donepezil (Aricept)

Mechanism of action: prevent breakdown of acetylcholine

-enhances transmission in cholinergic synapses

-only slows progression of disease

Prototype drug: benztropine mesylate (Cogentin)

Mechanism of action: acetylcholine receptor antagonists

-inhibits overactivity in brain

Primary use: used in early stages of disease

Prototype drug: levodopa (Larodopa)

Mechanism of action: increase availability of dopamine; restore balance of dopamine and acetylcholine

Primary use: used in later treatment of Parkinson's disease

Prototype drug: cyclobenzaprine (Flexeril)

Mechanism of action: inhibits upper-motor neuron activity

-causes CNS depression, alters simple spinal reflexes

Primary use: to treat localized spasms

Adverse effects: CNS depression, hepatic toxicity, physical dependence, anticholinergic effects

Prototype drug: dantrolene (Dantrium)

Mechanism of action: interferes with release of calcium ions in skeletal muscle

Primary use: to relieve dystonias and leg cramps

Adverse effects: hepatic toxicity, muscle weakness, drowsiness, diarrhea