Pharmacology 181

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• Pharmacology 181
• CHAPTER 19
• Analgesics, Sedatives
• and
• Hypnotics
• Dr. Jay Shahed

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Analgesics

• Indication
• Relieve pain.
• Psychological
• Some individuals have a higher thresh hold to
  pain than others
• Race, Religion
• Physiological.
• Endorphins release

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OPIOID ANALGESICS

• OPIODS
• NONOPIODS
• ADJUVANT

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OPIODS

• Types
• Full/Pure Agonists
• Morphine ( Morphine Sulfate ).
• Fentanyl (Fentanyl Citrate)
• Vicodin (Hydrocodone with Acetaminophen).
• Percocet( Oxycodone with Acetaminophen)
• Percodan ( Oxycodone with Aspirin)
• Demerol ( Meperidine).

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• Partial Agonists
• mixed Agonist- antagonist
• Natural Agonists
• Morphine
• Synthetic Agonists
• Meperidine ( usually combined with Phenergan.

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Other Drugs

• Codeine
• Stadol ( Butorphanol )
• Darvocet ( Propoxyphene HCl with Acetaminophen).
• Darvon ( Propoxyphene HCl with Acetaminophen).
• Pentazocine ( Talwin )
• Sufentanil citrate ( Sulfenta ).

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• Indications
• Mild, Moderate and severe pain management
• Cancer pain
• Side effects
• Physical and emotional dependence
• Sedation
• Confusion
• Hypotension
• Euphoria, Headaches and Dizziness, Convulsion
• Agitation
• Respiratory depression
• N/V/D.

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• Contra indications
• Head Injury
• Hypothyroidism
• Hepatic and real disease
• COPD
• Pediatrics
• Elderly
• Pregnant and lactating females.

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• Interactions
• Alcohol
• Hypnotics and sedatives
• Muscle relaxants
• Antiemetics
• Antihypertensives
• Antiarrhythmics.

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OPIOIDS ANTAGONISTS

• NALAXONE ( NARCAN)
• NALTREXONE ( REVIA )
• Indication
• Used to avoid relapses after withdrawal
• Caution
• Can lead into life threatening withdrawal

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NONOPIOD analgesics Antipyretics

• Some are available OTC.
• Relieve mild to moderate pain
• Fever
• Anti-inflammatory reactions

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Drugs

• Acetylsalicylic acid ( ASA )
• Aspirin, ASA
• Empirin
• Ascriptin
• Bufferin
• Acetaminophen
• Tylenol
• Datril
• Tempra

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• Combinations
• Anacin
• Equagesic
• Excedrin
• Parafon Forte
• Ultram

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Salicylates

• Indications
• Analgesia ( Pain)
• Anti - inflammatory
• Mechanism
• Prevent the formation of Prostaglandins.

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• Side effects
• Prolonged bleeding times, bruising
• Ulcers
• Tinnitus
• Hepatic and renal dysfunction
• Euphoria
• Dizziness
• Depression
• GI distress,
• Respiratory distress
• Poisoning and Coma

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• Contraindications
• Ulcers
• Bleeding disorders
• Asthma
• Pregnancy and lactation.
• Caution
• Anemia
• Pre-op and post- op
• Hepatic and renal disease.

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• Interactions
• Alcohol
• Anticoagulants
• Cimetadine
• Methotrexate
• Sulfonamides

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ACETAMINOPHEN

• Drug
• Tylenol
• No anti-inflammatory action
• Indication
• Pain and fever
• No anti-inflammatory effect
• Side effects
• Rash, Urticaria
• Liver toxicity
• Renal insufficiency.

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Tramadol ( Ultram ).

• Indication
• Centrally acting synthetic analgesic
• Inhibit the reuputake of Norepinephrine and
  Serotonin.
• Side effect
• Dizziness, Somnolence,Malaise
• Headaches
• N/V
• Sweating
• Pruritis
• Orthostatic Hypotension
• Anxiety, Confusion

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• Contraindication
• Head injuries
• Renal hepatic diseases
• Seizures
• Pregnancy
• Children under 16
• Caution
• Elderly
• Driving or operating machinery
• May impair mental ability
• Interactions
• MAO inhibitors
• Carbamazepine ( Tegretol )

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Adjunct Analgesics

• Tricyclic Antidepressant Drugs
• Amitripytline ( Elavil )
• Nortriptyline ( Palmelor )
• Imipramine ( Tofranil )

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• Indication
• Insomnia.
• Depression
• Nerve pain
• Herpes
• DM
• Cancer
• Migraine and tension headaches

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• Side effects
• Dry mouth
• Urinary retention
• Delirium
• Constipation
• Sedation
• Orthostatic Hypotension
• Heart blocks
• Tachyarrhythmias

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• Caution
• Prostatic Hypertrophy
• Urinary retention
• ICP
• Glaucoma
• Contraindications
• Hypersensitivity
• Myocardial infarction

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Anticonvulsants

• Drugs
• Carbamazine (tegetol)
• Phenytoin sodium (Dilantin)
• Indication
• Nerve pain ( Neuralgia)
• Herpes
• Cancer

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• Side effects
• Sedation, dizziness,confusion
• GI disturbance
• Hypotension
• Rash
• Steven Johnson syndrome.
• Severe allergic reaction to the drug
• Bullae, skin ulcers, pneumonia, joint pain,
  perforation of the cornea.
• Bone marrow suppression
• Nystagmus, Diplopia, Blurred vision.

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• Caution
• Hepatitis
• Renal disease
• Cardiac disease

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• Contraindications
• Bradycardia
• Pregnancy
• Adams -Stokes syndrome.
• Incomplete heart- block accompanied with
  seizures.
• Bone marrow depression
• Interactions
• Alcohol
• Antihistamines
• Antiacids
• Antineoplastic
• CNS depressants
• Folic Acid
• Dilantin

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Sedatives and Hypnotics

• Classification
• Barbiturates
• Non - Barbiturates

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Barbiturates

• Drugs
• Amobarbital (Amytal)
• Secobarbital (Seconal)
• Phenobarbital ( Nembutal )
• Talbutal ( Lotusate)

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• Indication
• Promote sedation in smaller doses
• Calmness and smooth muscle relaxation.
• Promote sleep in larger doses ( Hypnotic)
• depression of REM sleep.
• Treatment of seizure disorders
• (combined with Phenytoin Dilantin )

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• Side effects
• Dependency
• Hangover effect
• Depression
• Incoordination
• GI disturbance
• Rash, angioedema
• Coma.
• Long term use
• Rebound effect of nightmares and hallucinations.

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• Contraindication
• Not to be used with alcohol, overdose may be
  possible and can be fatal.
• Interactions
• Increase CNS depression
• Alcohol
• Monoamine Oxidase Inhibitors
• Sedatives
• Analgesics
• Decrease effects
• Oralcontraceptives(
• Corticosteroids
• Theophyline.
• Oral anticoagulants

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Non Barbiturates

• Drugs
• Choral hydrate (Noctec).
• Flurazepam (Dalmane)
• Triazolam (Halicon)
• Temazepam ( Rostril )
• Zolpidem Tartrate ( Ambien)

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• Indication
• These are safer than barbiturates
• Have a lesser potential for abuse.
• If miss used can lead to death
• Side effects
• Amnesia
• Confusion
• GI disturbance
• Rash
• Vertigo and ataxia.

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• Contraindications
• Elderly and children
• Renal and hepatic impairment
• Pregnant and lactating females
• Suicidal risk patients.
• Interactions
• Alcohol
• Antiemetics
• Antihistamines
• Analgesics.

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• Pharmacology 181
• Musculoskeletal
• and
• Anti- inflammatory drugs
• CHAPTER 21

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Skeletal muscle relaxants

• Drugs
• Caisoprodol ( Soma )
• Cyclobenzaprine ( Flexeril )
• Clorzaxazone ( Parafon Forte ).
• Diazepam ( Valium )
• Methocarbamol ( Robaxin ).
• Dantrolene ( Dantium ).
• Used for spasticity due to upper motor neurons

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• Indication
• Myalgia
• Muscle spasm
• Abnormal contractions and impaired mobility
• Backache
• Neck strain
• Acute pains are treated with
• Muscle relaxants NSAIDs
• Rest
• Physiotherapy
• Ice/Heat application

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• Caution
• Muscle relaxants can have an effect on the entire
  CNS therefore creating a sedative action as well
  as that of muscle relaxation.

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• Side Effects
• Respiratory arrest
• CNS problems
• Drowsiness, dizziness and xerostoma, Cephalgia,
  confusion, slurred speech
• Blurred vision
• Hypotension
• GI distress.
• Contraindications
• Muscular Dystrophy
• Myasthenia gravis
• Pregnancy and lactation
• Children.

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• Caution
• Hx of substance abuse
• Asthma
• Hepatic and renal disorders.
• Interactions
• Alcohol
• Analgesics
• Antihistamines.

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Anti inflammatory drugs

• Indication
• Arthritis
• Spondylitis
• Bursitis
• Gout
• Strains and sprains.
• Limited immobility

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NSAIDs

• Drugs
• Ibuprofen (Motrin, Advil)
• Diclofenac ( Voltaren )
• Indomethacin (Indocin)
• Ketoralac (Toradol)
• Sulindac (Feldene)
• Naproxen ( Naprosyn )
• Piroxicam ( Feldene )
• Sulindac ( Clinoril ).

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• Mechanism
• Inhibit the production of prostaglandins
• Indication
• Responsible for inflammations
• Sprains
• Menstrual cramps
• Rheumatic disorders.
• Osteoarthritis.

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• Side effects
• Ulceration with GI disturbance
• Caution
• Take with food or milk
• Avoid the use of aspirin,
• Immediately notify health care workers of
  presence of bleeding.
• Epigastric pain
• Tinnitus
• Cephalgia
• Hematuria
• Rash
• Increased bleeding time
• Hepatotoxicity.

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• Contraindications
• Asthma
• Cardiovascular disorders Gastroesophageal reflux
  disorder ( GERD ).
• Interactions
• Alcohol
• Anticoagulants
• Corticosteroids.

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Gout Medications.

• Pathophysiology
• Metabolic disorder that causes the accumulation
  of uric acid crystals with the joint space.
• Drugs
• Colchicine (Colchicine)
• Allopurinol ( Zyloprim )
• Mechanism
• Decrease uric acid levels in blood

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• Indication
• Anti-inflammatory
• Side effects
• Rash
• GI distress
• Blood disorders.

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Osteoporosis Therapy

• Drugs
• Alendronate (Fosmax)
• To be taken with 8 oz of water with calcium and
  Vitamin D supplementation
• Alcohol and nicotine restriction and no lying
  down for 30 minutes.Exercise therapy is advised.
• Action
• prevents reabsorption of bone minerals therefore
  increasing the mineral content within the bone.

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• Side effects
• GI distress
• Muscle pain
• Contraindications
• Renal disorders.
• Caution
• Upper GI disorders
• GERD and ulcers.