Pharmacology

Drugs Acting on the CNS and PNS

1. Anxiolytic and Hypnotic Agents
2. Anesthetics (General and Local)
3. Anticonvulsant Agents
4. Psychotherapeutic
5. Antidepressant Agent
6. Nonnarcotic and Narcotic Analgesics
7. Anti-parkinsonism
8. Muscle relaxants
9. Neuromuscular Blocking Agents
 Antixiolytic and Hypnotic Agents
• Sedation – diminishes physical and mental
response.
• Hypnotic- instigation of sleep
MOA: Depresses CNS by promoting the
effectiveness of GABA receptors.
Classes:
1. Barbiturates
2. Benzodiazepines
 Barbiturates
• Barb • Side effects:
Nausea
• Classified into: Vomiting
 Short-acting – induce sleep (secobarbital, Diarrhea
pentobarbital) Lethargy
 Intermediate- acting – induce sleep Drowsiness
(amobarbital, aprobarbital, butabarbital) Hangover
Dizziness
 Ultrashort- acting – used as a general
Rash
anesthetic [thiopental sodium (pentothal)]
• Adverse Reaction:
 Long-acting – control seizures
Tolerance
(phenobarbital, mephobarbital) Hypotension
 Benzodiazepines
• -zepam and –zolam • Side effects:
• Hypnotics: flurazepam, temazepam, Drowsiness
Lethargy
triazolam, estazolan, quazepam. Hangover
• Antianxiety: lorazepam (Ativan), Dizziness
diazepam (Valium), oxazepam Light-headedness
(Serax) Nausea and Vomiting
Diarrhea
• Classfied as Schedule IV Disorientation
• Antidote for overdose: flumazenil Respiratory Distress
 Anesthetics
General Anesthesia- Depresses CNS, alleviate pain, cause
a loss of consciousness.
• Inhalation: nitrous oxide (laughing gas), ether,
halothane, methoxyflurane
• IV: (Barbiturates) thiopental sodium, methohexital
sodium
(Benzodiazepines) diazepam (Valium), midazolam
• Others: droperidol (Innovar), etomidate (Amidate),
ketamine HCl (Ketalar), propofol (Diprivan)
Local Anesthesia- pain control while the
client is conscious. For performing dental • Adverse effects:
procedures, sutures, minor surgery and Allergic reactions
Respiratory Arrest
some diagnostic procedure.
Arrhythmias /
• Short-acting (1/2- 1h) chloroprocaine Cardiac Arrest
(Nesacaine), procaine HCl (Novocaine) Convulsion
Hypotension
• Moderate-acting (1-3h) lidocaine
(Xylocaine), mepivacaine HCl
• Long-acting (3-10h) bupivacaine
(Marcaine), etidocaine (Duranest),
dibucaine HCl (Nupercainal)
 Anticonvulsant
MOA: Suppress the abnormal electrical impulses from • Adverse
the seizure, CNS depressants.
Effects:
Drugs:
Blood dyscrasias
• Hydantoins (phenytoin, mephenytoin, ethotoin)
Nausea/
• Long-acting barbiturates (phenobarbital, vomiting
mephobarbital, primidone)
Dizziness
• Succimides (ethosuximide) Drowsiness
• Oxazolidones (trimethadione) Phenytoin:
• Benzodiazepines (diazepam, clonazepam) Ataxia,
• Carbamazepine and valproate (valproic acid) hypotension
 Antipsychotics
• Treatment of psychotic symptoms in
schizophrenia, psychosis, tourette’s syndrome.
• MOA: Blocks dopamine HCl receptors in the CNS.
• Can be given orally, IM or IV.
Classes:
• Phenotiazines
• Nonphenotiazine
• Phenothiazines (-zine)
 Aliphatic – strong sedative effect, decrease BP, and may
cause moderate pseudoparkinsonism. (chlorpromazine,
triflupromazine)
 Piperazine – low sedative and strong antiemetic effect.
Cause stronger pseudoparkinsonism. (prochlorperazine,
acetophenazine, fluphenazine, perphenazine and
trifluoperazine.
 Piperidine – strong sedative effect, causes low
pseudoparkinsonism, low to mod effect on BP.
(thioridazine, mesoridazine)
• Nonphenothiazines – butyrophenone (-dol)
(haloperidol [Haldol]) potent antipsychotig drug.
• Side Effects:
-EPS (extrapyramidal syndromes)
• Dystonia (spasms of tongue, face, neck and back)
• Akathisia (restlessness, inability to sit still, foot-tapping)
• Pseudoparkinsonism (muscle tremors, rigidity)
• Dyskenisia (lip smaking, constant chewing movement)
-Anticholinergic effect – dry mouth, increase heart rate,
urinary retention, constipation.
-Drowsiness
-Decrease in BP
-Blood dyscrasias (blood cell disorders)
 Antidepressant
• Also called as mood elevators, used for depressive episodes
accompanied by feelings of hopelessness and helplessness.
• MOA: Increase the amount of brain monoamine
neurotransmitters (norepinephrine, serotonin, dopamine)
Four Classes:
– Tricyclic Antidepressants (TCA) or tricyclics
– Selective Serotonin Reuptake Inhibitors (SSRI)
– Atypical Antidepressants
– Monoamine Oxidase Inhibitors (MAOI)
1. Tricyclic Antidepressants (TCA) – frequently
prescribed drug used to treat major depression.
(amitriptyline, trimipramine, doxepin)
Side Effects: Orthostatic hypotension, sedation,
anticholinergic effect, cardiac toxicity and seizures.

2. Selective Serotonin Reuptake Inhibitors (SSRI) –

used for treating major depression, obsessive
compulsive, panic, phobias, PTSD and other anxiety
disorders. (fluoxetine, paroxetine, citalopram)
Side Effects: G.I distress, Insomnia, Sexual Dysfunction
3. Atypical Antidepressants –for major depression,
reactive depression and anxiety. (amoxapine,
bupropion, nefazodone, trazodone)

4. Monoamine Oxidase Inhibitors (MAOI) –

prescribed when client does not respond to TCA
(tranylcypromine sulfate, phenizine sulfate)
Side effects: CNS Stimulation (agitation,
restlessness,insomia), orthostatic hypotension and
anticholinergic effects.
 Nonnarcotic and Narcotic Analgesics
• Prescribed for the relief of pain, choice of drug depends on the severity of
pain.
• When tissue damage occur, injured cells releases chemical mediators such as
bradykinin, serotonin and prostaglandin that affect the pain receptors
(nociceptors).
Types of Pain:
1. Acute – sudden pain, responds to treatment
2. Cancer – caused by pressure or blockage
3. Chronic – pain persist greater than 6 months
4. Somatic – pain from skeletal muscles, ligaments and joints
5. Superficial – pain from skin and mucous membrane injury
6. Vascular – pain caused by vascular or perivascular conditions
7. Visceral – body organ pain
 Nonnarcotic Analgesic
Effective for dull, throbbing pin of headaches, dysmenorrhea, inflammation,
minor abrasions, muscular pain and mild to moderate arthritis.
• Salicylates and Nonsteroidal Antiinflammatory Drugs (NSAIDs)- have
analgesic effect, as well as an antipyretic and antiinflammatory action.
(aspirin, ibuprofen, naproxen, mefenamic acid)
MOA: Inhibits the production of prostaglandin
Side Effects: Gastric irritation, Excess bleeding (menstruation),
Hypersensitivity (tinnittus, vertigo, bronchospasm and urticaria)
• Acetaminophen (Paracetamol) - popular nonprescription drug taken to
relieve pain, discomfort and fever. (Tylenol, Panadol, Tempra,)
Adverse effects: hepatoxicity
 Narcotic Analgesics
• Prescribed for moderate to severe pain.
• Narcotics act on the CNS and does not only suppress pain
impulses but also suppress respirations and coughing
(antitussive effect).
• Opium was used as early as 350 BC to relieve pain.
• Side effects: nausea and vomiting, constipation, moderate
decrease BP, orthostatic hypotension, respiratory depression
(with high dose), urinary retention.
• Drugs: Morphine, Meperidine (Demerol), Codeine,
Oxycodone.
 Morphine – potent, effective against acute pain resulting
from MI, cancer, dyspnea resulting form pulmonary
edema. Used as a preoperative medication.
 Meperidine – synthetic narcotics, shorter duration of
action, given orally, IM and IV and used to alleviate
postoperative pain.
• Narcotic antagonist: naloxone, naltrexone HCl,
nalmefene
 Anti-parkinsonism
• Parkinsonism is caused by an imbalance of the
neurotransmitters dopamine and acetylcholine due to cellular
death in the midbrain.
• MOA: Increase dopamine bioavailability or antagonize
acetylcholine.
• Drugs: BALSA: Bromocripitine, Amantadine, Levodopa (L-
dopa), Seligiline, Antimuscarinics.
• Side Effects: Nausea and Vomiting, Dyskinesia, Arrhymthia,
 Muscle Relaxants
• Relieve muscular spasms and pain associated with trauma
injuries and spasticity from chronic debilitating disorders
(e.g MS, strokes, cerebral palsy, head and spinal cord
injuries)
• MOA: acts on the spinal cord to suppress muscular
hyperactivity .
• Drugs: diazepam, baclofen, tizanidine, dantrolene.
• Side effects: drowsiness, dizziness, lightheadedness,
headaches, N/V , diarrhea and abdominal distress.
 Neuromuscular Blockers
• Used for muscle paralysis during mechanical
ventilation or surgery.
• MOA: competitive antagonistic against acetylcholine.
• Drugs: (-cur) atracurium, mivacurium, pancuronium,
rocuronium, tubocurarine, vecuronium.
• Side effects: Hypotension, tachycardia,