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Nervous System

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

Amphetamine-Like Drugs for ADHD and Narcolepsy


4. Methylphenidate
 to increase a child’s attention span and cognitive performance
(e.g., memory, reading) and to decrease impulsiveness,
hyperactivity, and restlessness; decrease
 to treat narcolepsy and helps to correct ADHD
 controlled-substance schedule II drug
 twice a day before bfast and lunch; 30-45 mins before meals (bc
it may cause insomnia); 6 hrs or more before sleep
 Amphetamine-like drugs are considered more effective in
treating ADHD than amphetamines.
 Amphetamine-like drugs potentiates the action of CNS
stimulants, such as caffeine, and inhibits the metabolism of
some barbiturates, such as phenobarbital, leading to increased
blood levels and potential toxicity.
Anorexiants
 appetite suppressants for short-term use (4 to 12 weeks), but no
longer recommended
 Side Effects: nervousness, restlessness, irritability, insomnia, heart
palpitations, and hypertension
 Lipase inhibitors: drug of choice for weight loss

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

II. CNS Depressants


Sedative Hypnotics
A. Barbiturates
 primarily for sedation preoperatively
 for short-term treatment of insomnia
 for control of seizures, preoperative anxiety, and sedation
induction
1. Pentobarbital sodium
 hypnotic of choice until the introduction of benzodiazepines in
 The onset of action of pentobarbital is slower when administered
intramuscularly (IM) than when administered orally (PO).
 May cause hepatotoxicity when taken with acetaminohphen
2. Secobarbital sodium

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

III. General Anesthetics


A. Inhalation
 used to deliver general anesthesia.
 absorbed quickly, have a rapid action, and are eliminated rapidly
 combined with a barbiturate (e.g., thiopental), a strong analgesic
(e.g., morphine), and a muscle relaxant (e.g., pancuronium) for
surgical procedures.
 Side effects: respiratory depression, hypotension, dysrhythmias,
and hepatic dysfunction
1. Halothane
 introduced as a nonflammable alternative.
 Highly potent anesthetic. Rapid recovery. Could decrease blood
pressure. Has a bronchodilator effect. Contraindicated in
obstetrics.
 Recovery: 1 hour
2. Isoflurane
 Frequently used in inhalation therapy. Has a smooth and rapid
induction of anesthesia and rapid recovery. Could cause
hypotension and respiratory depression. Not to be used during
labor because it suppresses uterine contractions. Has minimal
cardiovascular effect.
 Recovery: 1 hour
3. Sevoflurane
 for induction and maintenance during surgery. May be given
alone or combined with nitrous oxide.
 Recovery: within minutes
4. Nitrous oxide (laughing gas)
 Rapid recovery. Has minimal cardiovascular effect. Should be
given with oxygen. Low potency.
 Recovery: within minutes
B. Intravenous Anasthetics
 for general anesthesia or for the induction stage of anesthesia.

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.

B.2. IV Nonbarbiturate Anesthetics


1. Midazolam
 Induction time: rapid
 induction and maintenance of anesthesia or conscious sedation
for minor surgery or procedures like mechanical ventilation or
intubation.
 sedated and relaxed but responsive to commands.
 For induction of anesthesia and for endoscopic procedures. IV
drug can cause conscious sedation. Avoid if cardiopulmonary
disorder is present.
2. Etomidate
 Induction time: rapid
 Used for short-term surgery, for induction of anesthesia, or with
a general anesthetic to maintain the anesthetic state.
3. Ketamine
 Induction time: rapid
 Used for short-term surgery or induction of anesthesia. Increases
salivation, blood pressure, and heart rate. May be used for
diagnostic procedures. Avoid with history of psychiatric
disorders.
4. Propofol
 Induction time: rapid
 induction and maintenance of anesthesia or conscious sedation
for minor surgery or procedures like mechanical ventilation or
intubation.
 sedated and relaxed but responsive to commands.
 supports microbial growth and may increase the risk for
bacterial infection
 For induction of anesthesia; may be used with general
anesthesia. Short duration of action. May cause hypotension and
respiratory depression. Pain can occur at injection site, so may
be mixed with a local anesthetic (lidocaine) to decrease pain.

IV: Local Anesthetic


A. Spinal Anesthesia
 requires that a local anesthetic be injected in the subarachnoid
space at the third or fourth lumbar space
 decrease in cerebrospinal fluid pressure caused by a leak of fluid at
the needle insertion point (headache)
1. Chloroprocaine
 Short-acting (1/2-1 hr); ester
 For infiltration, caudal, and epidural anesthesia. Onset of action
is 6 to 12 minutes
2. Lidocaine
 Moderate-acting (1-3 hr);Amide
 replace procaine, except in dental procedures
 rapid onset and a long duration of action, is more stable in
solution, and causes fewer hypersensitivity reactions than
procaine.
3. Mepivacaine
 Moderate-acting (1-3 hr);Amide
 For nerve block, infiltration, caudal, and epidural anesthesia.
May be used in dentistry.Prilocaine
4. Bupivacaine
 Long-acting (3-10 hr); Amide
 For peripheral nerve block, infiltration, caudal, and epidural
anesthesia.
 delivered via a Y-connector to both sides at a flow rate of
approximately 2 mL/h (catheter)

B. Muscle Relaxants (Adjunct to Anesthesia)


 relieve muscular spasms and pain associated with traumatic
injuries and spasticity from chronic debilitating disorders
 Spasticity results from increased muscle tone from hyperexcitable
neurons caused by increased stimulation from the cerebral
neurons or lack of inhibition in the spinal cord or at the skeletal
muscles
1. Atracurium
2. Succinylcholine
 For surgical skeletal muscle relaxation. Also used in
endoscopy and intubation.

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.

VIII. Anti-Parkinson’s Drugs


 Parkinsonism (Parkinson’s disease) is a chronic neurologic
disorder that affects the extrapyramidal motor tract (which
controls posture, balance, and locomotion)
 Parkinsonism is caused by imbalance of the neurotransmitters
dopamine (DA) and acetylcholine (ACh).
 Degeneration of dopamine (inhibitory; maintains control of
acetylcholine and its excitatory response. Excessive
acetycholine stimulates the release of GABA. Symptomatic
movement disorders of parkinsonism occur. Remaining striatal
neurons synthesize dopamine from levodopa and release
dopamine as needed
 Three Cardinal Symptoms: rigidity, tremors, and bradykinesia
 Pseudoparkinsonism - an adverse reaction to antipsychotic drugs
1. Benztropine Mesylate
 Anticholinergic - reduce the rigidity and some of the tremors
but have minimal effect on bradykinesia.
 treat drug-induced parkinsonism, or pseudoparkinsonism
 First group of drugs used to treat Parkinson’s disease before
levodopa and dopamine agonists were introduced
2. Ethopropazine HCl
3. Trihexyphenidyl HCl
 Anticholinergic - reduce the rigidity and some of the tremors
but have minimal effect on bradykinesia.
 treat drug-induced parkinsonism, or pseudoparkinsonism
 First group of drugs used to treat Parkinson’s disease before
levodopa and dopamine agonists were introduced
4. Amantadine
 Dopamine antagonist
 First used as an antiviral drug for influenza A. Decreases
symptoms of parkinsonism. Can be used for early treatment of
Parkinson’s disease, which could delay the necessity of
levodopa. Is effective in treating drug-induced parkinsonism,
and has fewer side effects than anticholinergics.
5. Carbidopa-Levodopa
 Dopaminergics
 Decreases symptoms of parkinsonism. Carbidopa, a
decarboxylase inhibitor, permits more levodopa to reach the
striatum nerve terminals (where levodopa is converted to
dopamine). With the use of carbidopa, less levodopa is
needed.
 Levidopa- first dopaminergic drug
 Carbidopa- inhibit the enzyme dopa decarboxylase

IX. Cholinesterase Inhibitors


 Alzheimer’s disease is an incurable dementia illness
characterized by chronic, progressive neurodegenerative
conditions with marked cognitive dysfunction
 no known cure for Alzheimer’s disease; approved
medications to treat Alzheimer’s disease symptoms include
acetylcholinesterase (AChE) inhibitors
 AChE is an enzyme responsible for breaking down ACh and
is also known as cholinesterase.
1. Edrophonium chloride
 A rapid onset short acting cholinesterase inhibitpr used in
cardiac arrhythmias and in the diagnosis of myasthenia gravis
; antidote ro curare principles
2. Neostigmine bromide
3. Pyridostigmine bromide

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