updated on
December 26, 2007
Drug Profiles Spring Semester
|
Antipsychotics
(Note: excess dopamine
in the mesolimbic-mesocortical region of the CNS is believed to cause psychosis.
Dopamine antagonists can reduce these symptoms).
| Drug: Chlorpromazine
(Thorazine ®) |
| Drug Class: antipsychotic (typical) |
| Mechanism of Action: blocks alpha1
& 5-HT2 > D2 >D1 receptors.
(Note: multiple receptor types are blocked
by most antipsychotic drugs). |
| Indications: psychosis, nausea/vomiting,
sedation, intractable hiccups, tetanus (adjunct), acute intermittent porphyria |
| Contraindications: drug hypersensitivity,
CNS depression, bone marrow depression, hypotension, Parkinsonism, hepatic
dysfunction, glaucoma |
| Side Effects: drowsiness, seizures,
agranulocytosis, aplastic anemia, thrombocytopenia, neuroleptic malignant
syndrome, tardive dsykinesia |
| Pharmacokinetics: PO, IM, Rectal,
metabolized in the liver, 30 hr half life |
| Major drug Interactions: antacids,
alcohol, blood pressure medications, anticoagulants, phenytoin |
| Notes: use caution when driving -
may cause dizziness. Use alcohol cautiously. |
| Reference:
www.rxlist.com |
| Drug: Haloperidol
(generic, Haldol ®) |
| Drug Class: antipsychotic |
| Mechanism of Action: blocks D2 >
D1 = D4 > alpha1 > 5-HT2 receptors |
| Indications: psychosis (schizophrenia),
Tourette's syndrome |
| Contraindications: drug hypersensitivity,
CNS depression, Parkinson's disease, prolonged
QT |
| Side Effects: extrapyramidal (Parkinson-like)
symptoms, tardive dyskinesia, torsade de pointes, orthostatic hypotension,
neuroleptic malignant syndrome |
| Pharmacokinetics: PO, IM. metabolized
in the liver, 24 hr half life. |
| Major drug Interactions: lithium (encephalopathic
syndrome), CNS depressants |
| Notes: use caution when driving -
may cause dizziness. Use alcohol cautiously. DO NOT Administer IV. |
| Reference: www.rxlist.com |
| Drug: Risperidone
(Risperdal ®) |
| Drug Class: antipsychotic |
| Mechanism of Action: blocks D2 &
5-HT2 receptors. Also blocks M, alpha1 & H1 receptors. |
| Indications: psychosis (schizophrenia),
dementia |
| Contraindications: drug hypersensitivity,
prolonged QT, renal or liver disease |
| Side Effects: insomnia, agitation,
anxiety, extrapyramidal symptoms, constipation, rhinitis |
| Pharmacokinetics: PO, metabolized
in the liver, 24 hr half life. |
| Major drug Interactions: carbamazepine,
clozapine, drugs used to treat Parkinson's Dx., antihypertensive drugs |
| Notes: Use caution when driving -
may cause dizziness. Use alcohol cautiously. |
| Reference: www.rxlist.com |
| Drug: Clozapine
(generic, Clozaril ®) |
| Drug Class: antipsychotic (atypical) |
| Mechanism of Action: blocks D4 &
alpha1 > 5-HT2 > D2 & D1 receptors. Also blocks M & H1 receptors |
| Indications: schizophrenia (resistant),
suicide risk reduction assoc. w/ schizophrenia |
| Contraindications: drug hypersensitivity,
renal or liver disease, heart disease, WBC <3500, myloproliferative disorders |
| Side Effects: Drowsiness/sedation,
dizziness/vertigo, headache, tachycardia, constipation, hypersalivation,
aspiration pneumonia, tremor, disturbed sleep, hypokinesia, seizures, agranulocytosis |
| Pharmacokinetics: PO, metabolized
in the liver, 12 hr half life. |
| Major drug Interactions: drugs suppressing
bone marrow function, benzodiazepines & psychotropic drugs |
| Notes: Use caution when driving -
may cause dizziness. Use alcohol cautiously. |
| Reference: www.rxlist.com |
| Drug: Olanzapine
(Zyprexa ®) |
| Drug Class: antipsychotic |
| Mechanism of Action: blocks 5-HT2
> D1 - D4 & alpha1 receptors. Also blocks M & H1 receptors |
| Indications: psychosis, bipolar disorder |
| Contraindications: drug hypersensitivity |
| Side Effects: drowsiness, flu syndrome,
increased salivation, nausea, tardive dyskinesia |
| Pharmacokinetics: PO, metabolized
in the liver, ~30 hr half life. |
| Major drug Interactions: antihypertensive
drugs, levodopa, dopamine agonists, carbamazepine (p-450 inducer) |
| Notes: Use caution when driving -
may cause dizziness. Use alcohol cautiously. |
| Reference: www.rxlist.com |
Antidepressants
| Drug:Amitryptyline
(Elavil ®) |
| Drug Class: antidepressant (tricyclic
amine) |
| Mechanism of Action: blocks
reuptake of norepinephrine & serotonin at nerve endings(therapeutic
effects); Na channel blocker, antimuscarinic, antihistamine, alpha receptor
blocker (Note: multiple mechanisms of action). |
| Clinical Indications: for the relief
of symptoms of depression. Endogenous depression is more likely to be alleviated
than are other depressive states. |
| Contraindications: MAOI's use w/in
14 days, acute recovery period after a myocardial infarction, drug hypersensitivity |
| Side Effects: drowsiness, dry mouth
& eyes, constipation, orthotstatic hypotension, mild tremor, sweating,
agitation, nausea, tinnitus, prolonged QRS,
at toxic doses - potentially fatal cardiac
arrhythmias. |
| Pharmacokinetics: Oral. Amitriptyline
is metabolized by N-demethylation and bridge hydroxylation. Virtually the
entire dose is excreted as glucuronide or sulfate conjugate of metabolites,
with little unchanged drug appearing in the urine. |
| Major drug Interactions: decongestants
& local anesthetics w/ sympathomimetics, antihypertensives, CNS depressants,
drugs metabolized by P450-2D6. Concomitant use of tricyclic antidepressants
with drugs that can inhibit cytochrome P450 2D6 may require lower doses
than usually prescribed for either the tricyclic antidepressant or the other
drug. |
| Notes: several weeks required for
therapeutic effect to appear. Concomitant use of MAOI's can cause potentially
fatal hyperpyretic crisis & seizures (serotonergic syndrome). Potentially
fatal toxicity includes disturbances of cardiac conduction (widening of
QRS) and arrhythmias. |
| Reference: www.rxlist.com |
| Drug: Imipramine
(Tofranil ®) |
| Drug Class: antidepressant (tricyclic
amine) |
| Mechanism of Action: blocks
reuptake of norepinephrine & serotonin at nerve endings(therapeutic
effects); Na channel blocker, antimuscarinic, antihistamine, alpha receptor
blocker |
| Clinical Indications: depression,
chronic pain, nocturnal enuresis (peds) |
| Contraindications: MAOI's use w/in
14 days, acute recovery period after a myocardial infarction, drug hypersensitivity |
| Side Effects: drowsiness, dry mouth
& eyes, constipation, orthotstatic hypotension, mild tremor, sweating,
agitation, nausea, tinnitus |
| Pharmacokinetics: PO, metabolized
in the liver (P450 - 2D6) 16 hr half life |
| Major drug Interactions: decongestants
& local anesthetics w/ sympathomimetics, antihypertensives, CNS depressants,
drugs metabolized by P450-2D6. |
| Notes: Several weeks required for
therapeutic effect to appear. Concomitant use of MAOI's can cause potentially
fatal hyperpyretic cirsis & seizures. Potentially fatal toxicity includes
disturbances of cardiac conduction (widening of QRS) and arrhythmias. |
| Reference: www.rxlist.com |
SSRIs
| Drug: Fluoxetine
(Prozac ®) |
| Drug Class: antidepressant |
| Mechanism of Action: Selective Serotonin
Reuptake Inhibitor |
| Indications: depression,
obsessive-compulsive disorder, bulimia nervosa, panic disorder |
| Contraindications: drug hypersensitivity,
MAOI w/in 14 days, caution if liver dx. or impared renal function, drugs
metabolized by P450-2D6. Alcohol can interfere with SSRI's
therapeutic effects. |
| Side Effects: chills, hemorrhage,
hypertension, increased appetite, nausea & vomiting, weight gain, agitation,
amnesia, confusion, sleep disorder |
| Pharmacokinetics: PO, metabolized
in the liver (P450-2D6), several day half life |
| Major drug Interactions: |
| Notes: norfluoxetine
metabolite is active w/ a ~8 day half life; active drug
persists for weeks after dosing is stopped. Several weeks required for therapeutic
effect to appear. Consider this if switching from fluoxetine to an MAOI. |
| Reference: www.rxlist.com |
| Drug: Citalopram
(Celexa ®) |
| Drug Class: antidepressant |
| Mechanism of Action: SSRI |
| Indications: depression |
| Contraindications: MAOI's w/in 14
days. Alcohol can interfere with SSRI's therapeutic effects. |
| Side Effects: tachycardia, postural
hypotension, migraine, increased salivation, flatulance, weight change,
impaired concentration, decreased libido, delayed orgasms, |
| Pharmacokinetics: PO, metabolized
by the liver (P450 - 3A4 & 2C19), 35 hr half life |
| Major drug Interactions: MAOI's, P450
CYP 3A4 & 2C10 inhibitors, other CNS acting drugs |
| Notes: serotonin syndrome can develop
with concurrent use with MAOI's, avoid abrupt withdrawal |
| Reference: www.rxlist.com |
| Drug: Sertraline
(Zoloft ®) |
| Drug Class: antidepressant |
| Mechanism of Action: SSRI |
| Indications: depression, obsessive-compulsive
disorder, panic disorder, post-traumatic stress, premenstrual dysphoriic
disroder, social anxiety disorder |
| Contraindications: MAOI's w/in 14
days. Alcohol can interfere with SSRI's therapeutic effects. |
| Side Effects: sexual dysfunction,
impotence, chest pain, hypertonia, hypoesthesia, increased appetite, myalgia,
rhinitis, tinnitus |
| Pharmacokinetics: PO, metabolized
by the liver, 23 hr half life |
| Major drug Interactions: MAOI's, other
CNS acting drugs |
| Notes: serotonin syndrome can develop
with concurrent use with MAOI's, avoid abrupt withdrawal |
| Reference: www.rxlist.com |
| Drug: Paroxetine
(Paxil®) |
| Drug Class: antidepressant |
| Mechanism of Action: SSRI |
| Indications: Treatment of major depressive
episodes, panic disorder with or without agoraphobia (as defined in DSM-IV),
obsessive-compulsive disorders (as defined in DSM-IV), and social anxiety
disorder (social phobia, as defined in DSM-IV). The Controlled Release is
only for depression |
| Contraindications: MAOI's w/in 14
days, alcohol use may interefere with it's clinical efficacy |
| Side Effects: sexual dysfunction,
impotence, headache, somnolence, insomnia, agitation, seizures tremor, anxiety,
activation of mania or hypomania, dizziness, nervousness |
| Pharmacokinetics: PO, metabolized
by the liver, 21-24 hr half life |
| Major drug Interactions: MAOI's, other
CNS acting drugs |
| Notes: serotonin syndrome can develop
with concurrent use with MAOI's, avoid abrupt
withdrawal (symptoms may be severe) |
| Reference: www.rxlist.com |
| Drug: Bupropion
(Wellbutrin ®) |
| Drug Class: antidepressant |
| Mechanism of Action: multi mechanism
(weak reuptake inhibitor for serotonin, norepinephrine & dopamine) |
| Indications: treatment of major depressive
episodes, smoking cessation. |
| Contraindications: MAOI's w/in 14
days, patients with a seizure disorder, patients with a current or prior
diagnosis of bulimia or anorexia nervosa because of a higher incidence of
seizures. Although bupropion is not metabolized by cytochrome P450IID6 (CYP2D6),
there is the potential for drug-drug interactions when bupropion is co-administered
with drugs metabolozied by this isoenzyme |
| Side Effects: dry mouth and insomnia,
agitation |
| Pharmacokinetics: PO, metabolized
by the liver (Cyt P450 2B6) , ~21 hr half life |
| Major drug Interactions: MAOI's, other
CNS acting drugs |
| Notes: serotonin syndrome can develop
with concurrent use with MAOI's, avoid abrupt withdrawal |
| Reference: www.rxlist.com |
| Drug: Nefazodone
(Serzone ®) |
| Drug Class: antidepressant |
| Mechanism of Action: multiple
mechanisms: inhibits neuronal uptake of serotonin and norepinephrine
and antagonizes central 5-HT2 receptors and alpha-1-adrenergic receptors
(which may cause postural hypotension). Produces none to slight anticholinergic
effects, moderate sedation, and slight orthostatic hypotension. |
| Indications: treatment of major depressive
episodes |
| Contraindications: use with caution
in clients with a recent history of MI, unstable heart disease and taking
digoxin, or a history of mania. Use with caution during lactation. |
| Side Effects: dizziness, insomnia,
agitation, somnolence, lightheadedness |
| Pharmacokinetics: PO, extensively
metabolized by the liver with less than 1% excreted unchanged in the urine. |
| Major drug Interactions: MAOI's, other
CNS acting drugs, use with cisapride or pimozide |
| Notes: serotonin syndrome can develop
with concurrent use with MAOI's. WARNING Cases of life-threatening
hepatic failure have been reported in patients treated with SERZONE |
| Reference: www.rxlist.com |
| Drug: Venlafaxine
(Effexor ®) |
| Drug Class: antidepressant |
| Mechanism of Action: multiple
mechanisms: a potent inhibitor of the uptake of neuronal
serotonin and norepinephrine in the CNS and a weak inhibitor of the uptake
of dopamine. Has no anticholinergic, sedative, or orthostatic hypotensive
effects. |
| Indications: treatment of depression.
Treat generalized anxiety disorder (extended-release product). |
| Contraindications: use with caution
with impaired hepatic or renal function, in clients with a history of mania,
and in those with diseases or conditions that could affect the hemodynamic
responses or metabolism. Use of alcohol. Lactation. |
| Side Effects: anxiety, nervousness,
insomnia, mania, hypomania, seizures, suicide attempts dizziness, somnolence,
tremors, abnormal dreams |
| Pharmacokinetics: PO, Hepatic metabolism.
The major metabolite--O-desmethylvenlafaxine (ODV)--is active. The drug
and metabolite are eliminated through the kidneys. t1/2, venlafaxine: 5
hr; t1/2, ODV: 11 hr. |
| Major drug Interactions: MAOI's. |
| Notes: serotonin syndrome can develop
with concurrent use with MAOI's. |
| Reference: www.rxlist.com |
| Drug: St.
John's wort (Hypericum Perforatum) |
| Drug Class: antidepressant? (OTC) |
| Mechanism of Action: unclear. One
theory is that Hypericum Perforatum inhibits monoamine oxidase (MAO) and
catechol methyl-transferase (COMT). Another is that it may raise the levels
of serotonin. Still another theory suggests that Hypericum lowers levels
of the stress hormone cortisol or affects GABA receptors in the brain. |
| Indications: mild
to moderate depression, anxiety |
| Contraindications: MAOI's w/in 14
days, pregnancy, history of photosensitivity |
| Side Effects: photosensitivity, drug
allergy |
Pharmacokinetics: oral administration |
| Major drug Interactions: important
drug interactions with oral contraceptives, warfarin, cyclosporin and theophylline.
Hypericum-containing products appear to induce
hepatic enzymes of the cytochrome P450 group. |
| Notes: the name Wort is thought to
be derived from the Old English word for plant. The origins of the designator
"St. John" might be attributable to it’s medicinal usage
by the Knights of St. John in Jerusalem to heal the wounds of Crusaders
or that it blooms around the Christian Feast of St. John. |
| Reference: www.rxlist.com |
MAO Inhibitors/Lithium
| Drug: Lithium
(Eskalith ®) |
| Drug Class: anti-manic, mood stabilizer |
| Mechanism of Action: alters
sodium transport in nerve and muscle cells and inhibits
the recycling of neuronal membrane phosphoinositides involved
in generation of second messengers. |
| Indications: to treat
the manic stage of bipolar disorder (manic-depressive illness) |
| Contraindications: patients with significant
renal or cardiovascular disease, severe debilitation or dehydration, or
sodium depletion since the risk of lithium toxicity is high in these patients. |
| Side Effects: thyroid enlargement,
diarrhea, vomiting, tremor, mild ataxia, drowsiness or muscular weakness,
leukocytosis. |
| Pharmacokinetics: the distribution
space of lithium approximates that of total body water.
Lithium is primarily excreted in urine with insignificant excretion in feces.
Renal excretion of lithium is proportional to its plasma concentration.
The half-life of elimination of lithium is approximately 24 hours. Lithium
decreases sodium reabsorption by the renal tubules which could lead to sodium
depletion. |
| Major drug Interactions:diuretic-induced
sodium loss may reduce the renal clearance of lithium and increase serum
lithium levels with risk of lithium toxicity. In some cases, lithium toxicity
has resulted from interactions between an NSAID
and lithium. Indomethacin and piroxicam have been reported
to increase significantly, steady state plasma lithium concentrations. ACE
inhibitors, such as enalapril and captopril, may substantially
increase steady-state plasma lithium levels. Concurrent use of calcium channel
blocking agents with lithium may increase the risk of neurotoxicity. Lithium
may prolong the effects of neuromuscular blocking agents. |
| Notes: lithium toxicity is closely
related to serum lithium levels, and can occur at doses close to therapeutic
levels (very narrow therapeutic index).
Early symptoms of lithium toxicity can usually be treated by reduction or
cessation of dosage of the drug and resumption of the treatment at a lower
dose after 24 to 48 hours. Can produce nephrotoxicity. |
| Reference: www.rxlist.com |
MAOIs
(Note: avoid concomitant use
with tyramine-containing foods & serotonergic drugs, such as SSRIs)
| Drug: Phenelzine
(Nardil ®) |
| Drug Class: antidepressant , MAO inhibitor |
| Mechanism of Action: MAO inhibitor
that prevents MAO from metabolizing biogenic amines. (Because this enzyme
is widely distributed throughout the body, diverse pharmacologic effects
can be expected to occur) |
| Indications: depression characterized
as atypical. Investigational: Alone or as an adjunct to treat bulimia
nervosa, agoraphobia with panic attcks, globus hystericus syndrome, and
chronic headache. |
| Contraindications: pheochromocytoma,
CHF, history of liver disease, abnormal LFTs. Use
with other sympathomimetic drugs due to the possibility
of hypertensive crisis. |
| Side Effects: dizziness, headache,
drowsiness, sleep disturbances (insomnia, hypersomnia), fatigue, weakness,
tremors, convulsions. Slight anticholinergic, sedative, and orthostatic
hypotensive effects. |
| Pharmacokinetics: onset: few days
to several months. Beneficial effects at doses of 60 mg/day may not be seen
for at least 4 weeks. Clinical effects of the drug may be observed for up
to 2 weeks after termination of therapy. |
| Major drug Interactions: use with
serotoninergic agents (e.g.,
dexfenfluramine, fluoxetine, fluvoxamine, paroxetine, sertraline, venlafexine)
may produce serious, sometimes fatal, reactions. Use with caution in combination
with antihypertensive drugs, including thiazide diuretics and beta-blockers,
due to the possibility of severe hypotensive effects. Consumption of tyramine-rich
foods. |
| Reference: www.rxlist.com |
| Drug: Tranylcypromine
(Parnate ®) |
| Drug Class: monoamine oxidase inhibitor, antidepressant |
| Mechanism of Action: MAO inhibitor
(MAO-A & MAO-B) with a rapid onset of action. |
| Indications: major depression without
melancholia. Not a 1st line drug. |
| Contraindications: tranylcypromine
should not be administered in combination with antihypertensive, diuretic,
antihistaminic, sedative or anesthetic drugs; bupropion, buspirone, dextromethorphan;
cheese or other foods with a high tyramine content; or excessive quantities
of caffeine. Tranylcypromine should not be administered to any patient with
a confirmed or suspected cerebrovascular defect or to any patient with cardiovascular
disease, hypertension or history of headache. |
| Side Effects: hypotension, anxiety,
agitation, insomnia, drowsiness, dizziness, dry mouth; or may report nausea,
diarrhea, abdominal pain, constipation, tachycardia, significant anorexia,
edema, palpitation, blurred vision, chills and impotence. |
| Pharmacokinetics: MAO activity recovers
in 3-5 days after drug withdrawal, half life 2-3 hrs (faster
recovery of MAO activity due to its weaker bond to the enzyme). |
| Major drug Interactions: tyramine
containing foods, drugs that increase serotonin levels. |
| Notes: the most important reaction
associated with tranylcypromine is the occurrence of hypertensive crises
which have sometimes been fatal. |
| Reference: www.rxlist.com |
| Drug: Selegiline
(Eldepryl ®) |
| Drug Class: monoamine oxidase inhibitor, antidepressant |
| Mechanism of Action:
irreversible MAO inhibitor selective for MAO-B. (Brain MAO
is mainly B, while intestinal MAO is mostly the A isoform). It may also
increase dopaminergic activity by an unclear mechanism. |
| Indications: depression, adjunct with
levodopa in the treatment of Parkinsonism’s disease. |
| Contraindications: severe toxicity
has been reported with selegiline is combined with SSRIs or TCAs; contraindicated
for use with meperidine (& possibly other opioids). |
| Side Effects: nausea, hallucinations,
confusion, depression, loss of balance, insomnia, orthostatic hypotension |
| Pharmacokinetics: the bioavailability
of selegiline is increased 3 to 4 fold when it is taken with food. the mean
elimination half-life of selegiline is two hours The major plasma metabolites
are N-desmethylselegiline, L-amphetamine and L-methamphetamine. |
| Major drug Interactions: the occurrence
of stupor, muscular rigidity, severe agitation, and elevated temperature
has been reported in some patients receiving the combination of selegiline
and meperidine. Severe toxicity has been reported with selegiline is combined
with SSRIs or TCAs. |
| Notes: MAO in the GI tract and liver
are primarily type A, selegiline is less likely
to cause cheese reaction (hypertensive crisis). |
| Reference: www.rxlist.com |
| Drug: Mocolbemide
(Manerix ®) |
| Drug Class: monoamine oxidase inhibitor, antidepressant |
| Mechanism of Action: short
acting (24 hrs duration) reversible inhibitor of MAO-A |
| Indications: relief from depression |
| Contraindications: severe toxicity
has been reported with combined with TCAs. |
| Side Effects: headache, insomnia,
dizziness, anxiety, nausea, tachycardia, hypotension, dry mouth, sweating. |
| Pharmacokinetics: following oral administration,
moclobemide was 98% absorbed from the gastrointestinal tract. Absolute bioavailability
was approximately 55% after single doses. Moclobemide was extensively metabolized,
95% of the administered dose was excreted in the urine. |
| Major drug Interactions: cimetidine
can double the plasma levels of moclobemide |
| Reference: http://www.nlm.nih.gov/medlineplus/druginfo/uspdi/500127.html |
Anxiolytics/Sedatives/Hypnotics
Benzodiazepines (most end
with "am)
| Drug Class: Benzodiazepines |
| Mechanism of Action: binds
to benzodiazepine receptors, enhances GABA effects, especially in the limbic
system, thalamus & hypothalamus (the
same mechanism applies for the other benzodiazepines that follow). |
| Side Effects: drowsiness,
fatigue, ataxia, thrombosis/phlebitis at site of injection |
| Pharmacokinetics: many benzodiazepines
have long half lives (e.g. diazepam t 1/2 is 20-80 hrs). They undergo various
types of hepatic metabolism (the type of metabolism & rates depend on
the individual drug). |
| Major drug Interactions: ethanol &
CNS depressants (increase depressant effects) |
| Drug Dependence & Withdrawal:
DEA schedule IV. These drugs can be habit forming & cause physiologic
dependence. The severity of withdrawal symptoms differs between individual
drugs & depends on the dose used prior to cessation of use. Drugs with
longer half-lives are eliminated slowly enough to accomplish a gradual withdrawal
with few physical symptoms. The use of drugs with short half-lives for hypnotic
effects may lead to signs of withdrawal even between doses. |
| Reference: Katzung's text |
| Drug: Diazepam
(Valium ®) - The
Prototype |
| Drug Class: anxiolytic, antiepileptic |
| Indications: anxiety, alcohol withdrawal,
muscle spasm, seizures |
| Contraindications: narrow angle glaucoma,
pregnancy |
| Reference: www.rxlist.com |
| Drug: Chlordiazepoxide
(Libritabs, Librium ®) |
| Drug Class: anxiolytic |
| Indications: symptomatic relief of
mild anxiety and tension
and for reduction of tension states that may accompany muscle spasm. I.V.
chlordiazepoxide is indicated for the relief of acute agitation and hyperactivity
(e.g., alcoholism, anxiety, hysterical and panic states, drug withdrawal
symptoms). |
| Contraindications: myasthenia gravis.
|
| Reference: www.rxlist.com |
| Drug: Alprazolam
(Xanax ®) |
| Drug Class: anxiolytic |
| Indications: management of anxiety
disorder and treatment of panic
disorder. |
| Major drug Interactions: alprazolam
interaction with drugs that inhibit metabolism via cytochrome P450 3A. Drugs
that inhibit this metabolic pathway may have a profound effect on the clearance
of alprazolam. |
| Reference: www.rxlist.com |
| Drug: Flurazepam
(Dalmane ®) |
| Drug Class: hypnotic |
| Indications: insomnia. |
| Contraindications: known hypersensitivity
to benzodiazepines. Since clinical investigations of flurazepam have not
been carried out in children, currently it is not recommended for use in
children under 15 years of age. |
| Pharmacokinetics: flurazepam is rapidly
absorbed from the gastrointestinal tract and is rapidly metabolized. Because
of the long half-life of this metabolite (47 to 100 hours), peak hypnotic
effect of flurazepam may be reached after 2 to 3 nights of use. |
| Reference:
www.rxlist.com |
| Drug: Clonazepam
(Klonopin ®) |
| Drug Class: benzodiazepine, antiseizure |
| Indications: useful alone or as an
adjunct in the treatment of the Lennox-Gastaut syndrome (petit mal variant),
akinetic and myoclonic seizures. In patients with absence seizures (petit
mal) who have failed to respond to succinimides, clonazepam may be useful. |
| Pharmacokinetics: Cytochrome P-450,
including CYP3A, may play an important role in clonazepam reduction and
oxidation. |
| Reference: www.rxlist.com |
| Drug: Flumazenil (Romazicon
®) |
| Drug Class: benzodiazepine receptor
antagonist |
| Mechanism of Action: antagonizes
the actions of benzodiazepines |
| Indications: flumazenil is indicated
for the complete or partial reversal of the
sedative effects of benzodiazepines in cases where general
anesthesia has been induced and/or maintained with benzodiazepines, where
sedation has been produced with benzodiazepines for diagnostic and therapeutic
procedures, and for the management of benzodiazepine overdose. |
| Contraindications: patients with a
known hypersensitivity to flumazenil or benzodiazepines. Patients who have
been given a benzodiazepine for control of a potentially life-threatening
condition. Patients who are showing signs of serious cyclic antidepressant
overdose. |
| Side Effects: convulsions, dizziness,
injection site pain, increased sweating, headache, and abnormal or blurred
vision |
| Note: not recommended as a treatment
for benzodiazepine dependence. |
| Reference: www.rxlist.com |
| Drug: Lorazepam
(Ativan ®) |
| Drug Class: anxiolytic – sedative |
| Indications: the short-term relief
of manifestations of excessive anxiety in patients with anxiety
neurosis. |
| Contraindications: Myasthenia gravis,
acute narrow angle glaucoma, known hypersensitivity to benzodiazepines.
Lorazepam injectable is also contraindicated in patients with known hypersensitivity
to polyethylene glycol, propylene glycol or benzyl alcohol. |
| Reference: www.rxlist.com |
| Drug: Temazepam
(Restoril ®) |
| Drug Class: hypnotic |
| Indications: short-term management
of insomnia. |
| Contraindications: hypersensitivity
to benzodiazepines and in myasthenia gravis. |
| Side Effects: dizziness, lethargy,
drowsiness, confusion, euphoria, staggering, ataxia, falling. |
| Reference: www.rxlist.com |
Newer Non-Benzodiazepine Sleep Aids
| Drug: Zaleplon
(Sonata ®) |
| Drug Class: hypnotic |
| Mechanism of Action: a non-benzodiazepine
hypnotic. Its effect is believed to result from its interaction
with GABA-receptor complexes at binding domains located close to or allosterically
coupled to benzodiazepine receptors. (Zaleplon binds selectively to the
brain omega-1 receptor situated on the alpha subunit of the GABAA/chloride
receptor/channel complex.) It is chemically unrelated to benzodiazepines
& barbiturates. FWIW: chemically it is a member of the pyrazolopyrimidine
class of hypnotics. |
| Indications: for the short-term
treatment of insomnia. Sonata should be taken immediately
before bedtime or after the patient has gone to bed and has experienced
difficulty falling asleep. Sonata has been shown to decrease the time to
sleep onset for up to 30 days in controlled clinical studies. It has not
been shown to increase total sleep time or decrease the number of awakenings.
Hypnotics should generally be limited to 7 to 10 days of use, and reevaluation
of the patient is recommended if they are to be taken for more than 2 to
3 weeks. Sonata should not be prescribed in quantities exceeding a 1-month
supply. Sonata should be taken immediately before bedtime or after the patient
has gone to bed and has experienced difficulty falling asleep |
| Pharmacokinetics: rapidly eliminated
with a half life of ~1 hr.
Primarily metabolized by aldehyde oxidase. |
| Side Effects:increased incidence of headache
with higher doses. |
| Notes: its shorter duration of action causes less confusion
& tiredness on awakening; it may be a
safer drug to take if you have to ambulate (get up and walk around) at night.
|
| Reference:
www.rxlist.com |
| Drug: Zolpidem
(Ambien ®) |
| Drug Class: hypnotic |
| Mechanism of Action: Zolpidem interacts preferentially
with a subset of GABA-BZ1 receptor complexes and shares some of the pharmacological
properties of the benzodiazepines. FWIW: chemically it is a imidazopyridine
(chemically different from zaleplon & eszopiclone). Chemically unrelated
to benzodiazepines & barbiturates. |
| Indications: short-term
treatment of insomnia |
| Pharmacokinetics: Elimination half
life of ~2.5 hrs. |
| Reference:
www.rxlist.com |
| Drug: Eszopiclone
(Lunesta ®) |
| Drug Class: hypnotic |
| Mechanism of Action: interaction with GABA-receptor complexes
at binding domains located close to or allosterically coupled to benzodiazepine
receptors. FWIW: Chemically it is a pyrrolopyrazine derivative. |
| Indications: short-term
treatment of insomnia. It decreases sleep latency and improves sleep maintenance.
It should be taken immediately before bedtime. |
| Pharmacokinetics: eliminated with
a mean half life of approximately 6 hours. |
| Side Effects: somnolence (drowsiness) |
| Reference:
www.rxlist.com |
| Drug: Ramelteon
(Rozerem ®) |
| Drug Class: hypnotic |
| Mechanism of Action: a
melatonin receptor agonist with both high affinity for melatonin
MT1 and MT2 receptors and selectivity over the MT3 receptor. The activity
of ramelteon at the MT1 and MT2 receptors is believed to contribute to its
sleep-promoting properties, as these receptors, acted upon by endogenous
melatonin, are thought to be involved in the maintenance
of the circadian rhythm underlying the normal sleep-wake cycle.
Ramelteon has no appreciable affinity for the GABA receptor complex or for
receptors that bind neuropeptides, cytokines, serotonin, dopamine, noradrenaline,
acetylcholine, and opiates. |
| Indications: for the treatment of
insomnia characterized by difficulty with sleep onset. |
| Side Effects: mild and rare (so far
– it is a new drug). |
| Pharmacokinetics: CYP1A2 is the major
isozyme involved in the metabolism of ramelteon. The major metabolite of
ramelteon, M-II, is active and has approximately one tenth and one fifth
the binding affinity of the parent molecule for the human MT1 and MT2 receptors,
respectively, and is 17 – 25-fold less potent than ramelteon in in
vitro functional assays. Although the potency of M-II at MT1 and MT2 receptors
is lower than the parent drug, M-II circulates at higher concentrations
than the parent producing 20 – 100 fold greater mean systemic exposure
when compared to ramelteon. |
| Reference: www.rxlist.com |
Others
| Drug: Phenobarbital
(Solfoton ®) |
| Drug Class: antiepileptic, sedative |
| Mechanism of Action:
Potentiates GABAnergic stimulus by increasing the duration of GABA-gated
Cl channel openings. At high concentrations barbiturates
may directly activate Cl channels. The binding sites for barbiturates are
different from that of the benzodiazepines. Compared
to benzodiazepines, barbiturates are less selective in their actions
since they also depress the actions of excitatory neurotransmitters (e.g.
glutamate) and exert non-synaptic membrane effects in parallel with their
effects on GABA neurotransmission. This multiplicity of sites of action
may be the basis for their ability to induce full surgical anesthesia, and
for their more pronounced CNS depressant effects, which result in their
lower margin of safety compared to benzodiazepines.
|
| Indications: sedation,
hypnosis, anesthesia, epilepsy. |
| Contraindications: contraindicated
in the presence of glaucoma or prostatic hypertrophy. |
| Side Effects: depression of cardiac
and respiratory systems, cough, laryngospasm, bronchospasm. |
| Pharmacokinetics: long plasma half-life
(>60 h). Strong induction of microsomal enzymes. |
| Major drug Interactions: phenobarbital
reduces the effect of antipyrine, cimetidine, chlorpromazine, haloperidol,
nortriptyline, bishydroxycoumarin and warfarin. Valproic acid (Depakote)
can increase phenobarbital accumulation which can ultimately lower valproic
acid levels. Phenytoin (Dilantin) can cause an elevation in phenobarbital
levels. Other drugs can affect or be affected by phenobarbitol |
| Notes: phenobarbital may be habit
forming |
| Reference: www.rxlist.com |
| Drug: Buspirone
(BuSpar ®) |
| Drug Class: anxiolytic |
| Mechanism of Action: a partial
agonist of the 5-HT1A serotonin receptor.
|
| Indications: short-term symptomatic
relief of excessive anxiety
in patients with generalized anxiety disorder. |
| Contraindications: Avoid concomitant
use of other CNS agents, use of MAOIs may be hazardous (elevation of blood
pressure). |
| Side Effects: dizziness, headache,
drowsiness and nausea |
| Pharmacokinetics: buspirone is rapidly
absorbed in man and undergoes extensive first pass metabolism. Following
oral administration, low peak plasma levels of unchanged drug, of 1 to 6
ng/mL were observed 40 to 90 minutes after a single 20 mg dose. Buspirone
is metabolized primarily by oxidation, producing several hydroxylated derivatives
and a pharmacologically active metabolite, |
| Major drug Interactions: no sedation
or additive effects with EtOH. |
| Reference: www.rxlist.com |
| Drug: Hydroxyzine
(Atarax ®) |
| Drug Class: hypnotic |
| Mechanism of Action: atarax is unrelated
chemically to the phenothiazines, reserpine, meprobamate, or the benzodiazepines.
Atarax is not a cortical depressant, but its action may be due to a suppression
of activity in certain key regions of the subcortical area of the central
nervous system. |
| Indications: for symptomatic
relief of anxiety and tension associated with psychoneurosis
and as an adjunct in organic disease states in which anxiety is manifested.
Useful in the management of pruritus due to allergic conditions such as
chronic urticaria and atopic and contact dermatoses, and in histamine-mediated
pruritus. As a sedative when used as pre-medication and following general
anesthesia. |
| Contraindications: previous hypersensitivity
to the drug |
| Side Effects: usually mild and transitory
in nature, hypersedation |
| Pharmacokinetics: hydroxyzine is rapidly
absorbed from the gastrointestinal tract and Atarax's clinical effects are
usually noted within 15 to 30 minutes after oral administration. |
| Major drug Interactions: hydroxyzine
may potentiate meperidine (Demerols®) and barbiturates, so their use
in pre-anesthetic adjunctive therapy should be modified on an individual
basis. Can potentiate the effects of other CNS depressants. |
| Reference: www.rxlist.com |
Drugs of Abuse
Psychostimulants
| Drug: Caffeine
|
| Drug Class: CNS Stimulant, Methylxanthine |
| Mechanism of Action: Adenosine
receptor antagonist (leading to an increase in intracellular
cAMP) |
| Indications: Sleep retardant,
migraine, apnea of prematurity |
| Contraindications: none |
| Side Effects: Mild delirium, insomnia,
diuresis, dehydration, tachycardia and fever commonly occur with overdosage;
more serious overdosage can cause cardiac arrhythmias and clonic-tonic convulsions. |
Pharmacokinetics: Oral, IM or slowly
by IV. Half-life 6 hrs. |
| Major drug Interactions: none |
| Reference: www.rxlist.com |
| Drug: Nicotine
(Nicotrol ®) |
| Drug Class: CNS Stimulant |
| Mechanism of Action: nicotinic agonist.
A stimulating effect is exerted mainly in the cortex via the locus ceruleus
and a reward effect is exerted in the limbic system. At low doses the stimulant
effects predominate while at high doses the reward effects predominate |
| Indications: aid
to smoking cessation for the relief of nicotine withdrawal
symptoms |
| Contraindications: Inhaler therapy
is contraindicated in patients with known hypersensitivity or allergy to
nicotine or to menthol |
| Side Effects: Few & minor if used
as indicated. (Nicotine overdose: pallor, cold sweat, nausea, salivation,
vomiting, abdominal pain, diarrhea, headache, dizziness, disturbed hearing
and vision, tremor, mental confusion, and weakness) |
Pharmacokinetics: onset of CNS
effects occurs within seconds when inhaled in cigarrette smoke. |
| Major drug Interactions: may alter
the pharmacokinetics of certain concomitant medications, such as tricyclic
antidepressants and theophylline. |
| Reference:
www.rxlist.com |
| Drug: Cocaine
|
| Drug Class: CNS Stimulant |
| Mechanism of Action: blocks
monoamine reuptake transport into nerve terminals; Na channel
blocker |
| Indications: topical anesthesia of
the upper respiratory tract (due to its combined vasoconstrictor & local
anesthetic properties); use in EM as an ingredient in TAC (tetracaine, adrenaline
& cocaine) prior to wound cleaning & suturing. |
| Contraindications: hypersensitivity
to ester anesthetics, |
| Side Effects: signs of toxicity (overdosage)
include signs of CNS stimulation, tachycardia, hypertension, hyperthermia,
mydriasis, cardiac arrhythmias, seizures |
Pharmacokinetics: a topical local
anaesthetic; Half life is ~50 min. As a drug of abuse the HCl can be sniffed,
taken orally or injected IV. The base form (crack or freebase) is typically
smoked. |
| Major drug Interactions: MAOI inhibitors
would be expected to increase cocaine's effects & toxicity. Ethanol
consumption will convert cocaine to cocaethylene,
a derivative that has a half life of 3-4 hours and shares a similar pharmacology
as cocaine. Most cocaine abusers consume ethanol to prolong their high.
This may also increase cocaine's cardiotoxicity. |
| Notes: One of the most addictive drugs
known (Schedule II). |
| Reference: www.rxlist.com |
| Drug: Methylphenidate
(Ritalin ® or Concerta ® ) |
| Drug Class: mild CNS Stimulant |
| Mechanism of Action: May act by blocking
the reuptake mechanism of dopaminergic neurons |
| Indications:children with attention-deficit
disorders, methylphenidate causes decreases in motor
restlessness with an increased attention span. In narcolepsy
the drug acts on the cerebral cortex and subcortical structures
(e.g., thalamus) to increase motor activity and mental alertness and decrease
fatigue |
| Contraindications: marked anxiety,
tension and agitation, glaucoma. Use with caution during lactation. Use
with great caution in clients with history of hypertension or convulsive
disease. |
| Side Effects: nervousness, insomnia,
headaches, dizziness, drowsiness, chorea, nausea, anorexia, weight loss
|
Pharmacokinetics: oral tablets.
Peak blood levels, children: 1.9 hr for tablets (Ritalin
®), and 4.7 hr for extended-release tablets (Concerta
®). Duration: 4-6 hr. t1/2: 1-3 hr. Metabolized by the liver
and excreted by the kidney. |
| Notes: Schedule II drug with abuse
potential |
| Reference: www.rxlist.com |
| Drug: Dextroamphetamine
(Dexedrine ® ) |
| Drug Class: CNS Stimulant |
| Mechanism of Action: increases the
release of monoamines (norepinephrine, 5-HT
and dopamine) from their storage sites in nerve terminals,
competes with monoamines for reuptake, weakly inhibits MAO. Stronger CNS
effects and weaker peripheral action than amphetamine; thus, dextroamphetamine
manifests fewer undesirable CV effects |
| Indications: attention-deficit
disorders, narcolepsy. |
| Contraindications: lactation. Use
for obesity. |
| Side Effects: nervousness, insomnia,
palpitations, hypertension, hyperpyrexia, headaches, dizziness, anorexia,
weight loss, dryness of the mouth |
Pharmacokinetics: PO, completely
absorbed in 3 hr. Duration: PO, 4-24 hr; t1/2, adults: 10-12 hr; children:
6-8 hr. Excreted in urine. Acidification will increase excretion, while
alkalinization will decrease it. |
| Major drug Interactions: MAO inhibitors
will increase effects & toxicity |
| Notes: schedule II drug with high
abuse potential |
| Reference: www.rxlist.com |
| Drug: Methamphetamine
(Desoxyn & Gradumet ® ) |
| Drug Class: CNS Stimulant |
| Mechanism of Action: increases the
release of monoamines (norepinephrine, 5-HT and dopamine) from their storage
sites in nerve terminals, competes with monoamines for reuptake, weakly
inhibits MAO. Stronger CNS effects and weaker peripheral action than amphetamine;
thus, dextroamphetamine manifests fewer undesirable CV effects |
| Indications: attention-deficit
disorders in children over 6 years of age. Short
term treatment for obesity (use controversial and often
not recommended). |
| Contraindications: chronic use (more
than a few weeks) for obesity. Attention-deficit disorders in children less
than 6 years of age. |
| Side Effects: nervousness, insomnia,
palpitations, hypertension, hyperpyrexia, headaches, dizziness, anorexia,
weight loss, dryness of the mouth |
Pharmacokinetics: t1/2: 4-5 hr,
depending on urinary pH. Excreted in urine. Acidification will increase
excretion, while alkalinization will decrease it. |
| Major drug Interactions: MAO inhibitors
will increase effects & toxicity |
| Notes: schedule II drug with high
abuse potential |
| Reference: www.rxlist.com |
| Drug: Pemoline
(Cylert ® ) |
| Drug Class: CNS Stimulant |
| Mechanism of Action: believed to act
by dopaminergic mechanisms. Causes a decrease in hyperactivity and a prolonged
attention span in children. Has minimal sympathomimetic effects. Structurally
dissimilar to amphetamines & methylphenidate. |
| Indications: attention-deficit disorders.
Due to possible life-threatening hepatic failure, not
usually first-line therapy. Investigational: Narcolepsy.
|
| Contraindications: patients with known
hypersensitivity or idiosyncrasy to the drug. Should not be administered
to patients with impaired hepatic function. |
| Side Effects: symptoms of acute overdosage
result principally from overstimulation of the central nervous system and
from excessive sympathomimetic effects - e.g. similar to amphetamines |
Pharmacokinetics: pemoline is rapidly
absorbed from the gastrointestinal tract, Approximately 50% is bound to
plasma proteins. The serum half-life of pemoline is approximately 12 hours.
Peak serum levels of the drug occur within 2 to 4 hours after ingestion
of a single dose. |
| Major drug Interactions: use with
caution drugs with other CNS stimulants |
| Notes: DEA schedule IV. Possible life-threatening
hepatic failure has been associated with its use. |
| Reference: www.rxlist.com |
| Drug: MDMA
(ecstasy, X) |
| Drug Class: Drug of Abuse (CNS Stimulant &
hallucinogen) |
| Mechanism of Action: Causes the release
of serotonin, dopamine & norepinephrine. Reported to
produce a distorted sense of time & perception,
to facilitate interpersonal communication
& act as a sexual enhancer. |
| Indications: None. DEA Schedule I. |
| Contraindications: |
| Side Effects: Tachycardia, hypertension,
hyperpyrexia, mydriasis. Regular use is believed to produce long
term neurotoxicity (decreased number of serotonergic neurons
in multiple regions in the CNS). |
| Notes: DEA schedule I. |
| Reference:
http://www.drugabuse.gov/drugpages/mdma.html |
Hallucinogens
| Drug:
D-lysergic acid diethylamide (LSD, acid) |
| Drug Class: hallucinogen, drug of abuse |
| Mechanism of Action: agonist
and/or antagonist at 5-HT receptor subtypes. |
| Clinical Indications: none (a DEA
schedule I drug) |
| Side Effects: Mental:
delusions and visual hallucinations. The user's sense
of time and self may change. Sensations may seem to "cross
over," giving the user the feeling of hearing colors and seeing sounds.
These changes can be frightening and can cause panic. Physical:
dilated pupils, higher body temperature, increased heart rate and blood
pressure, sweating, loss of appetite, sleeplessness, dry mouth, and tremors |
| Pharmacokinetics: PO, very potent
dosage of 1-2 ug/kg; sold on the street in tablets, capsules, and, occasionally,
liquid form |
| Major drug Interactions: |
| Notes: panic attack can be managed
by “talking down” the patient, or with barbiturates or benzodiazepines;
Schedule I drug. |
| Reference: http://www.nida.nih.gov/infofax/lsd.html |
| Drug: Phencyclidine
(PCP, Angel dust) |
| Drug Class: hallucinogen (dissociative anesthetic),
drug of abuse |
| Mechanism of Action: poorly understood;
it blocks NMDA-type glutamate receptors &
may have other actions. |
| Clinical Indications: none (a DEA
schedule I drug) |
| Side Effects: acute
psychosis, dissociation, disorientation,
loss of proprioception, sweating,
numbness, nystagmus, rapid heart rate, hypertension, catatonic
posturing, aggressive behavior, hypersalivation in high
doses may cause coma (that may last up to 7-10 days), seizures or death |
| Pharmacokinetics: PO, IV, or smoked
|
| Notes: most common, and most dangerous,
hallucinogen; Schedule I Drug |
| Reference: http://www.drugabuse.gov/Infofax/pcp.html |
| Drug: Ketamine
(Ketalar ®) |
| Drug Class: hallucinogen (dissociative anesthetic),
drug of abuse |
| Mechanism of Action: poorly understood;
they block NMDA-type glutamate receptors
& may have other actions. |
| Clinical Indications: the sole anesthetic
agent for diagnostic and surgical procedures that do not require skeletal
muscle relaxation |
| Side Effects: similar to PCP (see
above) - catatonia, amnesia, analgesia, elevated heart rate, cardiac output
& blood pressure, post-op disorientation, sensory & perceptual illusions,
vivid dreams |
| Pharmacokinetics: parenteral |
| Notes: Schedule III Drug |
| Reference: www.rxlist.com
& Katzung's text |
| Drug: D9-tetrahydrocannabinol
(THC) |
| Drug Class: hallucinogen, antiemetic, analgesic,
drug of abuse |
| Mechanism of Action: cannabinoid
receptor agonist at CB1 and CB2 |
| Clinical Indications: amelioration
of nausea/ vomiting associated with cancer, appetite stimulation among AIDS
patients, chronic pain |
| Side Effects: few in the short term,
but can lead to an amotivational syndrome
with chronic use |
| Pharmacokinetics: PO, metabolized
in the liver, 6 hr halflife |
| Notes: clinical indications are based
on solid scientific research, but remain controversial. |
| Reference: http://www.drugabuse.gov/Infofax/marijuana.html |
Drug Tolerance & Dependence
| Drug: Cocaine
|
| Drug Class: CNS Stimulant |
| Mechanism of Action: blocks monoamine
reuptake transport into nerve terminals; Na channel blocker |
| Indications: topical anesthesia of
the upper respiratory tract (due to its combined vasoconstrictor & local
anesthetic properties); use in EM as an ingredient in TAC (tetracaine, adrenaline
& cocaine) prior to wound cleaning & suturing. |
| Contraindications: hypersensitivity
to ester anesthetics |
| Side Effects: signs of toxicity (overdosage)
include signs of CNS stimulation, tachycardia, hypertension, hyperthermia,
mydriasis, cardiac arrhythmias, seizures |
Pharmacokinetics: a topical local
anaesthetic; Half life is ~50 min. As a drug of abuse the HCl can be sniffed,
taken orally or injected IV. The base form (crack or freebase) is typically
smoked. |
| Major drug Interactions: MAOI inhibitors
would be expected to increase cocaine's effects & toxicity. Ethanol
consumption will convert cocaine to cocaetylene, a derivative that
has a half life of 3-4 hours and shares a similar pharmacology as cocaine.
Most cocaine abusers consume ethanol to prolong their high. This may also
increase cocaine's cardiotoxicity. |
| Notes: One of the most addictive drugs
known (Schedule II). |
| Reference: www.rxlist.com |
| Drug: Phenobarbital
(Solfoton ®) (barbiturates) |
| Drug Class: antiepileptic, sedative |
| Mechanism of Action: potentiates GABAnergic
stimulus. Inhibits Ca2+ channels. Block AMPA receptors. |
| Indications: management of simple
partial seizures and tonic-clonic seizures. |
| Contraindications: contraindicated
in the presence of glaucoma or prostatic hypertrophy. |
| Side Effects: depression of cardiac
and respiratory systems, cough, laryngospasm, bronchospasm. |
| Pharmacokinetics: long plasma half-life
(>60 h). Strong induction of microsomal enzymes. |
| Major drug Interactions: phenobarbital
reduces the effect of antipyrine, cimetidine, chlorpromazine, haloperidol,
nortriptyline, bishydroxycoumarin and warfarin. Valproic acid (Depakote)
can increase phenobarbital accumulation which can ultimately lower valproic
acid levels. Phenytoin (Dilantin) can cause an elevation in phenobarbital
levels. Other drugs can affect or be affected by phenobarbitol |
| Notes: phenobarbital may be habit
forming |
| Reference: www.rxlist.com |
| Drug: Morphine
(opioids) |
| Drug Class: narcotic analgesic |
| Mechanism of Action: opioid mu-receptor
agonist |
| Indications: pain relief |
| Contraindications: drug hypersensitivity |
| Side Effects: constipation, nausea,
vomiting, dizziness, sedation, respiratory depression, circulatory depression,
apnea, shock |
| Pharmacokinetics: PO, Transdermal,
Rectal. Metabolized in the liver, 2-4 hr half life |
| Major drug Interactions: other CNS
depressants |
| Notes: can cause psychological &
physical dependence |
| Reference: www.rxlist.com |
Drug Laws
DEA Schedule I (examples):
Drugs with a high potential
for abuse & no accepted therapeutic indication
| Drug: Phencyclidine
(PCP, Angel dust) |
| Drug Class: Hallucinogen (dissociative anesthetic),
drug of abuse |
| Mechanism of Action: poorly understood;
it blocks NMDA-type glutamate receptors & may have other actions. |
| Clinical Indications: none |
| Side Effects: Acute psychosis, dissociation,
disorientation, loss of proprioception, sweating, numbness, nystagmus, rapid
heart rate, hypertension, catatonic posturing, aggressive behavior, in high
doses may cause coma (that may last up to 7-10 days), seizures or death |
| Pharmacokinetics: PO, IV, or smoked
|
| Major drug Interactions: |
| Notes: Most common, and most dangerous,
hallucinogen; Schedule I Drug |
| Reference: http://www.drugabuse.gov/Infofax/pcp.html |
| Drug: Heroin
(diamorphine, diacetylmorphine) (street names:
"smack," "H," "skag," "junk") |
| Drug Class: hallucinogen , drug of abuse |
| Mechanism of Action: Similar to morphine.
Heroin is a central nervous system depressant that relieves pain and induces
sleep. It produces a dreamlike state of warmth and well-being. It may also
cause constricted pupils, nausea, and respiratory depression, which in its
extremes can result in death. Heroin activates brain regions that produce
euphoric sensations and brain regions that produce physical dependence :
hence its notorious ability to produce both psychological and physical addiction.
With regular heroin use, tolerance develops. |
| Clinical Indications: none |
| Side Effects: Withdrawal symptoms
include panic, nausea, muscle cramps, chills, and insomnia. Heroin use during
pregnancy increases the risk of miscarriage and stillbirth |
| Pharmacokinetics: PO, IV, or smoked.
The short-term effects of heroin abuse appear soon after a single dose and
disappear in a few hours. |
| Major drug Interactions: |
| Notes: Schedule I Drug. Heroin is
processed from morphine, a naturally occurring substance extracted from
the seedpod of the Asian poppy plant. Heroin abuse is associated with serious
health conditions, including fatal overdose, spontaneous abortion, collapsed
veins, and infectious diseases, including HIV/AIDS and hepatitis. |
| Reference: http://www.drugabuse.gov/Infofax/heroin.html |
DEA Schedule II (example):
Drugs with a high potential
for abuse & accepted therapeutic indications (no refills)
| Drug: Cocaine
|
| Drug Class: CNS Stimulant |
| Mechanism of Action: blocks monoamine
reuptake transport into nerve terminals; Na channel blocker |
| Indications: topical
anesthesia of the upper respiratory tract (due to its combined
vasoconstrictor & local anesthetic properties); use in EM as an ingredient
in TAC (tetracaine, adrenaline
& cocaine) prior to wound cleaning & suturing. |
| Pharmacology: see Drugs
of Abuse. One of the most addictive drugs known |
| Reference: www.rxlist.com |
DEA Schedule III (example):
Drugs with recognized
abuse potential by not as great as those above (5 refills/6 month limit)
| Drug: Testosterone
|
| Drug Class: Androgen |
| Mechanism of Action: binds to intracellular
androgen receptor & modulates gene expression. |
| Indications: replacement therapy
in males for congenital or acquired primary hypogonadism
or for congenital or acquired hypogonadotropic hypogonadism. Delayed puberty.
In postmenopausal women to treat inoperable metastatic breast carcinoma
or in premenopausal women following oophorectomy. Postpartum breast
engorgement (evidence for effectiveness is lacking). Investigational: Male
contraceptive (testosterone enanthate). |
| Notes: DEA schedule III. Abusers
use this drug to increase muscle mass & strength, not
to produce euphoria. |
| Reference: http://www.drugabuse.gov/Infofax/steroids.html |
DEA Schedule IV (example):
Drugs with less potential
for abuse (5 refills/6 month limit)
| Drug: Diazepam
(Valium ®) |
| Drug Class: anxiolytic, antiepileptic |
| Mechanism of Action: binds to benzodiazepine
receptors, enhances GABA effects, especially in the limbic system, thalamus
& hypothalamus |
| Indications: anxiety, alcohol withdrawal,
muscle spasm, seizures |
| Notes: IV injection should be made
very slowly, avoid alcohol, habit forming
(DEA schedule IV) |
| Reference:
www.rxlist.com |
DEA Schedule V (example):
Drugs with low potential
for abuse, prescription not required unless additional state regulations apply
| Drug: Codeine |
| Drug Class: narcotic analgesic |
| Mechanism of Action: opioid
agonist. The major effects of codeine are on the central
nervous system and the bowel. |
| Clinical Indications: For the relief
of mild to moderate pain |
| Notes: DEA Order Form Required for
prescriptions |
| Reference: www.rxlist.com |