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I. CNS Stimulants
A. Amphetamines/Anorexiants
Amphetamine:
1. Amphetamine SO4
stimulate the release of neurotransmitters— norepinephrine and
dopamine—from the brain and sympathetic nervous system
for narcolepsy and ADHD
euphoria, alertness, sleeplessness, restlessness, tremors,
irritability, dry mouth, diarrhea, constipation, and impotence
continuous use: increased heart rate, palpitations, cardiac
dysrhythmias, and increased blood pressure
HL: 4 to 30 hours
2. Dextroamphetamine SO4
3. Methamphetamine HCL
B. Analeptics
affect the brainstem and spinal cord but also affect the cerebral
cortex.
stimulate respiration
1. Caffeine
stimulates the CNS, and large doses stimulate respiration
Newborns with respiratory distress might be given caffeine to
increase respiration
Side effects:
nervousness, restlessness, tremors, twitching, palpitations,
insomnia, dieresis, GI irritation, and tinnitus
More than 300 mg of caffeine affects the CNS and heart
HL: 5 hours
2. Theophylline
used mostly to relax the bronchioles
increase respiration in newborns.
3. Doxapram
to treat respiratory depression caused by drug overdose,
preanesthetic and postanesthetic respiratory depression, and
chronic obstructive pulmonary disease (COPD)
to treat neonatal apnea
Mechanical ventilation is more effective than doxapram for
treating patients who experience respiratory depression as a result
of using certain drugs.
O: 20-40 secs; P: 2 minutes
Side Effects:
Infrequent
Overdose: hypertension, tachycardia, tremors, spasticity, and
hyperactive reflexes
B. Benzodiazepine
Selected benzodiazepines (minor tranquilizer or anxiolytic) were
introduced with chlordiazepoxide (Librium) in the 1960s as
antianxiety agents.
used to treat insomnia by inducing and sustaining sleep
increase the action of the inhibitory neurotransmitter gamma-
aminobutyric acid (GABA) to the GABA receptors (Neuron
excitability is reduced.)
1. Alprazolam
2. Flurazepam
C. Benzodiazepine Antagonist
1. Flumazenil
D. Nonbenzodiazepines
1. Zolpidem Tartrate
differs in chemical structure from benzodiazepines
metabolized in the liver to three inactive metabolites and is excreted
in bile, urine, and feces
B.1. IV Barbiturates
1. Thiopental sodium
ultrashort-acting barbiturate
general anesthetic used for short-term surgery
used for rapid induction stage of anesthesia and in dental
procedures.
2. Methohexital sodium
Induction time: rapid
Has short duration. Frequently used for induction and with other
drugs as part of balanced anesthesia. An inhalation anesthesia
usually follows.
3. Thiamylal sodium
Induction time: rapid
Used for induction of anesthesia and as anesthesia for electroshock
therapy.
IV. Anticonvulsants
A. Barbiturates
enhancing the activity of GABA
1. Amobarbital
2. Phenobarbital
long-acting barbiturate
treat partial seizures, grand mal seizures, and acute episodes
of status epilepticus seizures; meningitis; toxic reactions; and
eclampsia
may be used with combination to phenytoin
20 to 40 mcg/mL
B. Iminostilbene
1. Carbamazepine
effective in treating refractory seizure disorders that have not
responded to other anticonvulsant therapies
used for psychiatric disorders (e.g., bipolar disease), trigeminal
neuralgia (as an analgesic), and alcohol withdrawal
5 to 12 mcg/mL.
C. Valproate
1. Valproic acid
prescribed for petit mal, grand mal, and mixed types of
seizures
for psychomotor, myoclonic, absence, and tonic-clonic
seizures
50 to 100 mcg/mL.
D. Benzodiazepine (Anxiolytic)
Antidote: Flumazenil
1. Clonazepam
effective in controlling petit mal (absence)
seizures,myoclonus, and status epilepticus
may be used when petit mal seizure are refractory to
succinimides or valproic acid
2. Diazepam
primarily prescribed for treating acute status epilepticus;
inhibiting sodium influx, stabilizing cell membranes,
reducing repetitive neuronal firing, and limiting seizures.
3. Lorazepam
To control status epilepticus; also treats anxiety and
substance abuse withdrawal
E. Hydantoins
inhibiting sodium influx, stabilizing cell membranes, reducing
repetitive neuronal firing, and limiting seizures.
1. Phenytoin
first anticonvulsant used to treat seizures
most commonly used drug for controlling seizures
F. Miscelleaneous
1. Gabapentin
Adjunctive therapy for partial seizures
Promotes GABA release
2. Levetiracetam
For complex partial seizures
For adjunctive and monotherapy
Unlikely to cause drug interactions
3. Magnesium sulfate
To control seizures in toxemia of pregnancy caused by
eclampsia or preeclampsia
V. Narcotic Analgesics
A. Opioid Agonist-Antagonist
1. Nalpbuphine
To relieve moderate to severe pain
Inhibition of pain impulses transmittedin the CNS by binding
with opiate receptor and increasing threshold
2. Morphine
B. Opioid Analgesics
antidotes for overdoses of natural and synthetic opioid
analgesics
have a higher affinity to the opiate receptor site than the
opioid being taken
blocks the receptor and displaces any opioid that would
normally be at the receptor, inhibiting the opioid action.
1. Tramadol
2. Oxycodone HCL
VI. Antipsychotics
block the D2 (dopaminergic) receptor, which in turn promotes
the presence of EPS, resulting in drug-induced
pseudoparkinsonism in varying degrees
block the chemoreceptor trigger zone and vomiting (emetic)
center in the brain
When dopamine is blocked, however, extrapyramidal symptoms
(EPS) of parkinsonism may develop.
A. Phenothiazines
Block norepinephrine, causing sedative and hypotensive effects
early in treatment.
1. Chlorpromazine
first phenothiazine introduced for treating psychotic behaviour
aliphatic group- strong sedative effect, decreased blood
pressure, and may cause moderate EPS (pseudoparkinsonism)
may produce orthostatic hypotension
2. Fluphenazine
piperazine group- produce more EPS than other phenothiazines.
dry mouth, urinary retention, and agranulocytosis
rapid and not affected by food.
3. Prochlorpherazine maleate
B. Nonphenothiazides
block only the neurotransmitter dopamine
1. Haloperidol
Butyrophenone group
frequently prescribed nonphenothiazine
potent antipsychotic drug (0.5-5 mg)
C. Atypical Antipshychotics
effective in treating both positive and negative symptoms of
schizophrenia
Two advantages: treat negative symptoms and not likely to
cause EPS
have a greater affinity for blocking serotonin and dopaminergic
D4 receptors than primarily blocking the dopaminergic D2
receptor responsible for mild and severe EPS.
1. Risperidone
does not cause agranulocytosis
Paliperidone- major active metabolite of risperidone
2. Clozapine
first atypical antipsychotic agent used to treat schizophrenia
and other psychoses
only indicated for the treatment of severely ill schizophrenic
patients who have not responded to traditional antipsychotic
drug
may cause severe reactions such as seizures and
agranulocytosis
VII. Antidepressants
Antidote: Phentolamine
A. Tricyclic Antidepressants
used to treat major depression because they are effective and
less expensive than SSRIs and other drugs
block the uptake of the neurotransmitters norepinephrine and
serotonin in the brain
2 to 4 weeks of drug therapy; given at night
elevates mood, increases interest in daily living and activity, and
decreases insomnia
1. Amitriptyline HCl
For depression with or without melancholia
may lead to extrapyramidal symptoms (EPS)
2. Imipramine HCl
used for the treatment of enuresis (involuntary discharge of
urine during sleep in children).
For depression.
3. Nortriptyline HCl
For depression. Similar to imipramine HCl
major metabolites of imipramine and amitriptyline.
B. Selective Serotonin Reuptake Inhibitors
block the reuptake of serotonin into the nerve terminal of the
CNS, thereby enhancing its transmission at the serotonergic
synapse
do not block the uptake of dopamine or norepinephrine, and they
do not block cholinergic and alpha1-adrenergic receptors
for major depressive disorders and for treating anxiety disorders
such as obsessive-compulsive disorder, panic, phobias,
posttraumatic stress disorder, and other forms of anxiety.
popular antidepressants because they do not cause sedation,
hypotension, anticholinergic effects, or cardiotoxicity as do
many of the TCAs
1. Fluoxetine
To treat depression with or without melancholia
Serotonin and norepinephrine are increased in nerve cells
because of blockage from nerve fibers.
2. Sertraline HCl
the most commonly prescribed antidepressant among SSRIs
For major depressive disorders. Do not take with MAOIs or
TCAs.
C. Monoamide Oxidase Inhibitors
(MAO) inactivates norepinephrine, dopamine, epinephrine, and
serotonin. By inhibiting MAO, the levels of these
neurotransmitters rise.
MAO-A inactivates dopamine in the brain,
MAO-B inactivates norepinephrine and serotonin
not the antidepressants of choice; still used for mild, reactive,
and atypical depression (chronic anxiety, hypersomnia, fear).
1. Isocarboxacid
For depression that is refractory to TCAs.
2. Phenelzine Sulphate
For depression
3. Tranylcypromine Sulphate
For depression
D. Mood Stabilizer
treat bipolar affective disorder
1. Lithium carbonate
first drug used to manage this disorder
antimania drug that is effective in controlling manic behavior
that arises from underlying bipolar disorder.
first-line drugs for bipolar disorder
has a calming effect but may cause some memory loss and
confusion; controls any evidence of flight of ideas and
hyperactivity
therapeutic serum range: 0.5 to 1.5 mEq/L.