Antiseizure drug (act as GABA agonists), 

brand name: valium

used for generalized seizures- absence, tonic-clonic, and myoclonic

stimulate influx of chloride ions (effect associated with GABA),

delaying influx of sodium and calcium

excreted faster with a slightly acidic filtrate

Adverse effects: drowsiness, sedation, ataxia, laryngospasm, respiratory depression, cardio collapse, coma

• Therapeutic class: Anti-seizure drug; antidysrhythmic

• Pharmacologic class: hydantoin; sodium influx-suppressing drug

• Actions: desensitizes sodium channel in CNS that are responsible for neuronal responsivity; this prevents the spread of disruptive electrical charges in the brain that produce seizures

• Effective against most types of seizures, except absence seizures

Onset is slow and peak is 1.5-3 hrs for IR and 4-12 hrs for XR; duration is 15 days

Adverse effects:

• Dysrhythmias such as bradycardia or ventricular fibrillation

• Severe hypotension

• Hyperglycemia

• Headache, ataxia, confusion and slurred speech, twitching, insomnia

• Aplastic anemia

• Severe skin rashes, including exfoliative dermatitis and Stevens-Johnson syndrome

Contraindications:

• pts with hypersensitivity to hydantoin products

• Rash, seizures due to hypoglycemia, sinus bradycardia and heart block

Interactions:

• Oral anticoagulants, glucocorticoids, food supplements (folic acid, calcium & vitamin D)

• Should not be combined with tricyclic antidepressants

• Can increase serum levels of glucose and may decrease protein-bound iodine and urinary steroid levels

Lithium (Eskalith)

• Therapeutic class: bipolar mood stabilizer

• Pharm class: glutamate inhibitor, serotonin receptor antagonist

• Used in treatment for bipolar disorder

• Remains effective in purely manic and purely depressive states

• Narrow therapeutic/toxic ratio; risk of toxicity is high

• Onset is 5-7 days

• Acts like sodium in the body and conditions when sodium are lost (ie. excessive sweating or dehydration) can cause lithium toxicity

• Overdose may be treated with hemodialysis and supportive care & serum sodium and lithium level need to be monitored together

• Adverse effects:

• Headache, lethargy, fatigue, recent memory loss, nausea, vomiting, anorexia, abdominal pain, diarrhea, dry mouth, muscle weakness, hand tremors, reversible leukocytosis, nephrogenic diabetes insipidus

• Peripheral circulatory collapse

• This drug is contraindicated for Pts with renal disease, dehydration, cardiovascular disease and cases of severe sodium depletion

• First atypical antipsychotic (2nd generation)

• Control positive and negative schizophrenia

• no ESP effects

• may block D2 receptors and serotonin (5-HT) and alpha adrenergic receptors

• Adverse side effects of atypical antipsychotics:

• tachycardia, transient fever, sedation, dizziness, headache, lightheadedness, somnolence, anxiety, nervousness, hostility, insomnia, nausea, vomiting, constipation, parkinsonism, akathisia

• Clozapine brings increased risk of agranulocytosis

• Therapeutic class: conventional antipsychotic; schizophrenia drug

• First effective drug to treat schizophrenia

• Action: D2 dopamine receptor antagonist

• Can be administered PO (max dose: 1,000 mg/day), IV/IM (max dose: 600 mg every 4-6h)

• Adverse effects include:

• Common: drowsiness, dizziness, orthostatic hypotension, urinary retention

• Serious: agranulocytosis, pancytopenia, anaphylactoid reaction, tardive dyskinesia, neuroleptic malignant syndrome, hypothermia, adynamic ileus, sudden unexplained death

• Contraindicated in Pts with: alcohol withdrawal, comatose state, bone marrow depression, Reye’s syndrome or during lactation

• Lab tests: false-positives may be seen for urine bilirubin, pregnancy tests, or amylase

• Drug interactions:

• Avoid concurrent use with sedatives such as phenobarbital

• Taking with tricyclic antidepressants can elevate BP

• Taking it with antiseizure medications can lower the seizure threshold

• Therapeutic class: conventional antipsychotic; schizophrenia drug

• Action: D2 dopamine receptor antagonist, nonphenothiazine

• Pregnancy class C

• Used to treat Pts with Tourette’s syndrome and children with severe behavioral problems (unprovoked aggression or hyperexcitability)

• Long-lasting IM or subcutaneous administration - good for Pts who are uncooperative/unable to take oral meds

• *Do NOT abruptly discontinue; severe adverse reactions will occur

• Adverse effects:

• High incidence of extrapyramidal side effects (EPS) such as acute dystonia (muscle spasms of back, neck, tongue and face), akathisia (inability to rest/relax), parkinsonism (tremor, muscle rigidity, stooped posture, shuffling gait)  and tardive dyskinesia

• Older adults more likely to experience adverse effects, so they’re perscribed ½ adult dose

• Interactions:

• Decreased effect when combined with: lithium, phenobarbital, beta blockers

• Haloperidol inhibits action of centrally acting antihypertensives  

• therapeutic class: analgesic; antipyretic

• pharmacological class: centrally acting COX inhibitor

• mechanism of action

• reduces fever by direct action at the level of the hypothalamus and dilation of peripheral blood vessels which enables sweating and dissipation of heat

• used to treat

• useful in treatment of fever in children

• relief of mild to moderate pain when aspirin is contraindicated

• adverse effects

• AE are uncommon, generally safe drug

• less GI issues than aspirin

• toxicity can lead to renal failure

• inhibits Warfarin

• overdose treatment: N-acetylcysteine

• therapeutic class: analgesic; anti-inflammatory drug, antipyretic

• pharmacologic class: NASAID

• Uses:

• treatment of mild to moderate pain, fever, and inflammation

• common indications include pain associated with chronic musculoskeletal disorders such as RA, osteoarthritis, headache, dental pain, and dsymenorrhea

• Action: inhibition of prostaglandin synthesis

• Adverse effects

• mild nausea, heartburn, epigastric pain, dizziness

• GI ulceration with occult or gross bleeding may occur in high doses

• chronic use can lead to renal failure

• Interactions/Contradictions

• should be avoided when taking anticoagulants

• should be avoided with patients who have peptic ulcers

• Class: opioid analgesics

• Action: inhibits ascending pathways, altering perception response to pain

• Uses

• sometimes used to treat opioid addiction \

• methadone maintenance: treats opioid dependence; allows patient to return to productive work and social life without physical, emotional, and criminal risks

• heroin addicts switched to methadone to prevent unpleasant withdrawal symptoms

• prolonged withdrawal, less symptoms

• adverse effects

• dizziness, nausea, cardiac arrest, convulsions, severe respiratory depression or arrest

• anticholinergic effects  (dry mouth, palpitation, tachycardia)

• Anticholinergic drug - induces fight or flight responses by inhibiting parasympathetic response

• Used to treat irritable bowel syndrome (IBD)

• Taken orally

• Adverse effects:

• Dry mouth

• Blurred vision

• Drowsiness

• Constipation

• Urinary Hesitancy

• Tachycardia

• Class: Atypical Antipsychotic drug

• Treats schizophrenia and schizoaffective disorder by controlling both positive and negative schizophrenic symptoms

• Mechanism of action: dopamine system stabilizers/ domamine partial agonists

• Adverse effects are virtually non-existant although noticable side effects include:

• Headache

• Nausea/vomiting

• Fever

• Constiptation

• Anxiety

• opioid agonist

• Schedule I

• too dangerous for therapeutic use

• major drug of abuse

• After injection or inhalation, heroin rapidly crosses the blood brain barrier to enter the brain, where it’s metabolized to morphine.

• Activates mu and kappa receptors

• Initial effect -> intense euphoria (“rush”) followed by several hours of deep relaxation.

• Therapeutic class: centrally acting skeletal muscle relaxant

• Pharmaceutical class: catecholamine reuptake inhibitor

• Action: depresses motor activity in brainstem by increasing norepinephrine and blocking presynaptic uptake

• No used in pediatrics

• Pregnancy class B

• onset: 1 hour Peak: 3-8 hours Duration: 12-14 hours

• Adverse: drowsiness, blurred vision, dizziness, dry mouth, rash, tachycardia  

• OD: physostigmine

• Therapeutic class: Sedative-hypnotic

• Pharmacologic class: non-benzodiazepine GABA receptor agonist; non-barbiturate CNS depressant

• Actions: facilitates GABA-mediated CNS depression in limbic, thalamic, and hypothalamic regions

• Preserves stages III and IV of sleep

• Used for short-term insomnia management (7-10 days)

• Onset: rapid (7-27 minutes), should be given immediately before bedtime

• Pregnancy category B ** lactating women should not take this drug

• Adverse effects:

• Daytime sedation

• Confusion

• Amnesia

• Dizziness

• Depression

• Nausea/vomiting

• Interactions

• When taken with food, onset is delayed

• Increased sedation when used concurrently with other CNS depressants (including alcohol)

• Use flumazenil for overdose treatment

• Therapeutic class: antiparkinson

• Pharmacologic class: centrally acting cholinergic receptor blocker

• Action: blocking excess cholinergic receptor blocker

• can be taken in divided doses

• Onset: 15m IM/IV 1 hour PO Peak: 1-2 hours duration: 6-10 hours

• Pregnancy class C

• adverse: dry mouth, constipation, tachycardia, sedation, restlessness, irritability, nervousness, insomnia

• Contradicting: glaucoma, myasthenia gravis, GI obstruction

• OD: physostigmine

• Therapeutic: antiparkinson

• Pharmacological: dopamine precursor, dopaminergic

• restores dopamine in the extra pyramidal symptoms of the brain

• carbidopa and entacapone: prevent enzymatic breakdown of dopamine

• DO NOT STOP WITHOUT CONSULTING DOCTOR

• onset: 30min Peak: 1-2 hours Duration: Variable

• adverse effects: uncontrolled and purposeless movement, muscle twitching, shrugging, orthostatic hypotension

• contraindicated in patients with lesions on their skin or melanoma

• OD: general support measures

• Primary use: Incontinence

• Pharmacologic Class: Anticholinergic/ muscarinic antagonist

-Act by competing with Ach for binding muscarinic receptors. Suppressing the effects of Ach causes symptoms of sympathetic nervous system activation to predominate.

• Adverse effects for anticholinergics:

• tachycardia

• CNS stimulation

• urinary retention in men with prostate disorders

• Therapeutic class: Opioid analgesic

• Pharacologic class: opioid receptor agonist

• Actions: binds with mu and kappa receptor sites to produce profound analgesia

• Causes euphoria, constriction of pupils & stimulation of cardiac muscle

• Use:

• Symptomatic relief of serious acute and chronic pain (after non-narcotic analgesics have failed)

• Pre-anesthetic medication

• Relieves shortness of breath associated with heart failure and pulmonary edema

• Acute chest pain connected with MI

• Oral capsules should be taken whole; not broken, chewed, dissolved or crushed

• It is a Schedule II controlled substance & should be taken properly according to dispensing instructions ***

• Pregnancy category B (it is category D if used in high doses or for long periods of time)

• Onset: less than 60 minutes and can last up to 7 hours

• Adverse effects:

• Orthostatic hypertension (b/c it causes peripheral vasodilation)

• Dysphoria (restlessness, depression & anxiety)

• Hallucinations

• Nausea

• Constipation

• Dizziness

• Itching sensation

• Interactions

• Should be avoided with CNS depressants (alcohol, other opioids, general anesthetics and MAO inhibitor anti-depressants)

• Should be avoided in cases of acute or severe asthma, GI obstruction and severe hepatic or renal impairment

• IV administration of naloxone for over dose

• Therapeutic class: NSAID, non opioid, antipyretic

• Pharmacological Class: salicylate, cyclooxygenase inhibitor

• Inhibits prostaglandin synthesis causing vasodilation and anticoagulants

• Works by inhibiting both COX 1 and COX 2

• Excreted in urine causing skewed glucose tests

• Pregnancy class D

• Onset: 1 hour Peak: 2-4 hours Duration: 24 hours

• Adverse Effects: GI bleeding, enteric coated tablets available to lessen the amount released in stomach

• Do not combine with other anticoagulants  

• Pharmacologic class: benzodiazepine

• Intensify the effect of GABA in the brain.

• bind directly to the GABA receptor, suppressing abnormal neuronal foci

• Therapeutic class: antiseizure

• Indications: absence seizures and myclonic seizures

• absence seizure: generalized class

• lasting a few seconds

• seen most often in children (child stares into space, does not respond to verbal stimulation. may have fluttering eyelids or jerking)

• myclonic seizures: special syndromes class

• large jerking movements of a major muscle group, such as an arm

• falling from a sitting position or dropping what is held

• Route and Adult Dose

• PO; 1.5mg/day in three divided  doses, increased by 0.5-1mg every three days until seizures are controlled

• Adverse effects:

• drowsiness, sedation, ataxia

• laryngospasm, respiratory depression, cardiovascular collapse, coma

• Therapeutic class: Sedative-hypnotic; anxiolytic, anesthetic adjunct

• pharmacologic class: benzodiazepine; GABA-receptor agonist

• potentiating effects of GABA (inhibitory neurotransmitter) in thalamic, hypothalamic, limbic levels of CNS.

• this means that it stimulates influx of chloride ions; it also delays influx of sodium and calcium into neuron

• potent benzodiazepine

• half-life of 10-20 hours (once or twice a day oral dosing)

• anxiolytic, also used as preanesthetic medication to provide sedation and management of status epilepticus and tonic-clonic seizures

• also used for chemotherapy induced nausea and vomiting

• IV (4 mg injected slowly at 2 mg/min) for orally;

• AE: drowsiness, sedation, amnesia, weakness, disorientation, ataxia (lack of voluntary muscle control), sleep disturbance, blood pressure changes, blurred vision, nausea, vomiting.

• Antidote for overdose of Benzodiazepines (sedative-hypnotic)

• Pregnancy class C

• Adverse effects: nausea, dizziness, blurred vision, agitation, dyspnea, xerostomia,

• Therapeutic class: antiseizure drug; sedative

• Pharmacologic class: Barbiturate; GABA receptor agonist

• Actions: long-acting barbiturate that enhances the action of GABA neurotransmitter

• Use: management of variety of seizures, promotes sleep

• **** SHOULD NOT BE USED TO MANAGE PAIN- IT WILL INCREASE SENSITIVITY TO PAIN

• Pregnancy category D

• Schedule IV (high possibility of becoming dependent)

• Should NOT be given via IM injections - it can cause irritation to the soft-tissue

• Onset: 20-60 minutes

• Adverse effects:

• May cause dependence

• Drowsiness

• Vitamin deficiencies (vit. B; D; folate)

• Larygnospasms

• Contraindications: not to be used with severe uncontrolled pain, pre-existing CNS depression, severe respiratory disease with dyspnea or obstruction, glaucoma or prostatic hypertrophy

• Interactions:

• Not to be taken with alcohol or CNS depressants

• Phenobarbital increases the metabolism of many other drugs, reducing their effectiveness