ANALGESICS

I. Pain
 occurs when there is tissue damage

release of kinins & prostaglandins

stimulate sensory nerves (A-delta & C fibers)

pain is perceived

 Gate-Control Theory

II. Non -Narcotic Analgesics

A. Nonsteroidal Antiinflammatory Drugs (NSAIDs)

• ibuprofen (Advil, Alaxan, Dolan, Muskelax, Midol)
• mefenamic acid (Dolfenal, Gardan, Ponstan)
• Naproxen (Flanax)
• Ketorolac (Toradol)
• ketoprofen (Orudis)
• diclofenac (Cataflam, Neopyrazone )
• indomethacin
• piroxicam
• Meloxicam (Mobic)

Indic:
 analgesic (arthritis, mild-moderate pain, dysmenorrhea)
 antipyretic

MOA: block prostaglandin (PG) synthesis

Side Effects:
1. gastric irritation & bleeding -MC
2. blood dyscrasias
3. dizziness
4. hypotension
5. pruritus
6. Na & water retention
7. tinnitus

B. Salicylates
• aspirin (ASA, Aspilet)

Indic:
 analgesic
  antipyretic
 anticoagulant (reduce risk of TIA, stroke, or MI)
MOA: block PG synthesis

Side Effects:
1. gastric irritation
2. 8th CN damage
3. salicylism
a. tinnitus, dizziness
b. difficulty hearing
c. N, V & diarrhea
d. confusion
4. salicylate toxicity

C. Cyclooxygenase (COX)- 2 inhibitors

• celecoxib ( Celebrex )
• valdecoxib ( Bextra )

Indic:
 analgesic

MOA: block cyclooxygenase-2 ---> reduce inflammation & pain

Side Effect: less GI & CNS effects

D. Acetaminophen
• acetaminophen (Tylenol)

Indic:
 analgesic,
 antiypyretic

MOA: blocks PG synthesis

Side Effects:
1. V,A, N
2. rash
3. hepatotoxicity
4. acetaminophen toxicity

III. Narcotic (Opioid) Analgesics

• morphine
• meperidine (Demerol)
• nalbuphine (Nubain)
• codeine
 • oxycodone
• methadone
• Butorphanol (Stadol)
Indic:
 DOC for severe pain
 cough suppressant
 slows motility of GIT
 induction of anesthesia

MOA: bind with opioid receptors -->regulate transmission of pain impulses,

promote feelings of well-being & euphoria

Side Effects:
1. constipation
2. hypotension
3. urinary retention
4. miosis
5. respiratory depression
6. euphoria & sedation
7. drug tolerance & drug dependence
8. increase ICP

 Opioid Antagonist
• naloxone (Narcan)
• Naltrexone

Indic:
 reversal of opioid effects in narcotic overdose
 Dx of narcotic overdose

MOA: reverses opioid effects ( resp. depression, sedation & hypotension)

Side Effects:
1. Acute narcotic abstinence syndrome
 NV, sweating, tachycardia, hypotension
2. BP changes
3. pulmonary edema
 ANTIMIGRAINE DRUGS

I. Headaches
a. Migraine headache
i. Common migraine
ii. Classic migraine

b. Cluster headache
c. Tension headache

II. Ergot Derivatives

 ergotamine

Indic: prevent or abort migraine attacks in adults

MOA: not understood, constricts cranial blood vessels

Side Effects:
1. peripheral vasoconstriction (sometimes severe)
a. numbness, tingling in toes & fingers
b. muscle pain
c. pulselessness or weakness of legs
2. CV changes
3. ergotism
a. NV,
b. diarrhea
c. excessive thirst
d. hypoperfusion
e. chest pain
f. confusion

III. Triptans
 sumatriptan

Indic: tx of acute migraine

tx of cluster headache (Sub-Q route)

MOA: binds with serotonin receptors --> constricts cranial bld vessels

Side Effects:
same as ergots but less systemic effects

IV. others:
Propranolol – beta blocker
Side Effect : bradycardia, bronchospasm
 CNS STIMULANTS

I. Amphetamines
• amphetamine sulfate
• dextroamphetamine (Dexedrine)
• methylphenidate HCl (Ritalin)

Indic:
 Tx of narcolepsy
 Tx of attention deficit hyperactivity disorder

MOA: stimulate cerebral cortex

II. Anorexiants (Antiobesity )

• phentermine HCL (Ionamin , Duromine)
• benzphetamine HCl

Indic: simple obesity

MOA: act on cerebral cortex & hypothalamus --> suppress appetite

III. other CNS stimulants:

• aminophylline
• theophylline
• caffeine

Indic: tx of asthma

MOA: act on brainstem & medulla --> stimulate respiration

Side Effects of CNS stimulants:

1. irritability
2. restlessness & tremors
3. insomnia
4. heart palpitations & tachycardia
5. HPN
6. dry mouth
7. anorexia & weight loss
8. diarrhea or constipation
9. impotence
10. dependence & tolerance