Pharm Narcotics And Antimigraine Agents Ch 26 Karch

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Chapter 26

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Narcotics and Antimigraine Agents
Pain

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Pain Definition

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A sensory and emotional experience associated with accute or potential tissue damage
What ever the patient says it is

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Two types of drugs to relieve pain

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Narcotics
Antimigraine drugs

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Narcotics def

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Opium derivatives used to treat many types of pain

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Antimigraine drugs

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Reserved for the treatment of migraine headaches

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A-Delta fibers

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Fast mylenated nerve fibers stimulated by mechanical and thermal receptors. Generate sharp, acute, electric pain sensation that runs up to the thalamus

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C-fibers

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Slow fibers transmit burning, aching, throbbing.
Stimulated by chemicals - inflammation.
Terminate before the thalamus

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Gate Control Theory

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Transmission of information along the spinothalamic tracts can be modulated/blocked all along these tracts by other impulses traveling up and down.

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Pain Threshold

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The physical level of stimulation to nerve fibers required to produce the perception of pain

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Pain Tolerance

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The psychological component which determines the amount of pain a patient can endure wo interfering with normal function

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Opioids are therapeutic because they

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Occupy specific ipioid receptors in teh CNS

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Location of Opioid receptors throughout the body

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CNS-thalamus, hypothalamus,
Nerves in the periphery
GI Tract

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Brain stem opioid receptors are responsible for

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Blood pressure
Pupil diameter
GI secretions
Chemoreceptor Trigger Zone
controls nausea, vomiting, cough, respirations

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Spinal cord and thatamus receptors are responsible for

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Integrate and relate incoming ifnormation about pain

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In the hypothalamus receptors are responsible for

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Interrelating the endocrine and neural response to pain

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In the limbic system receptors are responsible for

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Emotional aspects and response to pain

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At peripheral nerve sites opioids may

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block the release of neurotransmitters related to pain and inflammation

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Narcotic agonist
Actions

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Act at specific opioid receptor sites in the CNS
Produce analgesia, sedation
Sense of well-being

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Narcotic agonist
Indications

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Relief of severe acute or chronic pain
Analgesia during anesthesia

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Narcotic agonist
Pharmacokinetics

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IV delivery most reliable for therapeutic response
IM and SubQ rate of absorption vary
Liver metabolized
Urine and bile excreted

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Narcotic agonist
Contraindications

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Known allergy to opioids
Pregnancy, labor, lactation
Diarrhea caused by poisons

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Narcotic agonist
Cautions

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Respiratory dysfunction
GI or
GU surgery
Acute abdomen and ulcerative colitis

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Narcotic agonist
Adverse reactions

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Respiratory depression with apnea
Shock
Orthostatic hypotension
Nausea, vomiting, constipation
Biliary spsm
Dizziness, psychosis, anxiety, fear, hallucinations

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Narcotic agonists
D's of adverse reactions

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Dizziness, drowsiness, Dependence, Decreased BP, Decreased peristalsis

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Narcotic agonist
Drug-Drug interactions

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Barbiturates as general anesthesia
Phenothiazines-anti-emetics
MAO's

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Narcotic agonist
Prototype

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morphine
Roxanol

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Narcotic Agonists-Antagonists
Prototype

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Stimulate certain opioid receptors but block other such receptors
pentazocine - Talwin

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Narcotic Agonists-Antagonists
Actions

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Bind to specific iopiod receptor sites in the CNS
Produce analgesia, sedation, euphoria, hallucinations

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Narcotic Agonists-Antagonists
Indications

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Moderate to severe pain
As an adjunct to general anesthesia
Relief of pain during labor and delivery

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Narcotic Agonists-Antagonists
Pharmacokinetics

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Readily absorbed IM
Quickly reach peak levels when given IV

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Narcotic Agonists-Antagonists
Contraindications

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Known allergy to Narcotic Agonists-Antagonists
During pregnancy and lactation

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Narcotic Agonists-Antagonists
Cautions

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Physical dependence to a narcotic
COPD and diseases of the respiratory tract rt respiratory depression
Acute MI and documented CAD

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Narcotic Agonists-Antagonists
Adverse reactions

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Respiratory depression
Nausea, vomiting, constipation, biliary spasm
Headache, Dizziness, Psychoses, Anxiety, Hallucinations
UReteral spasm and urinary retention

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Narcotic Agonists-Antagonists
Drug-Drug interactions

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Barbiturate general anesthetics

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Narcotic Antagonists
Prototype drugs

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Reverse the effects of narcotics
Revex, Narcan, ReVia

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Narcotic Agonists
Actions

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Drugs that bind strongly to opioid receptors but do not activate the receptor
Reverse the effects of opioids

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Narcotic Antagonists
Indications

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Reversal of the adverse effects of narcotics
Treat narcotic and/or alcoholic dependence

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Narcotic Antagonists
Pharmacokinetics

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Well absorbed IV, IM, SubQ
Widely distributed
Liver metabolized
Urine excreted
Enters breast milk

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Narcotic Antagonists
Contraindications

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Know allergy

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Narcotic Antagonists
Cautions

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Pregnancy and lactation
Narcotic addiction
CV disease

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Narcotic Antagonists
Adverse reactions

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Acute narcotic abstinence syndrome
CNS excitement
Tachycardia
BP changes
Arrhythmias

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Narcotic Antagonists
Adverse reactions
P's of blocking Opioid Agonists

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Increased
Perspiration
Pulse
Puke
Pain
Blood Pressure

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Narcotic Antagonists
Drug-Drug interactions

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Larger doses may be needed to reduce the effect of Antagonists-Agonists.

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Headaches
3 types of headaches

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Migraine
Cluster
Tension
Caused by vaso dilation

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Migraine headaches
Women

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Severe, throbbing headaches on one side of the head

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Cluster headaches
Men

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Begin during sleep, sharp, steady eye pain, sweatting, flushing, tearing, nasal congestion

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Tension headaches
Women

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Usually occur at times of stress; dull band of pain around the entire head

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Ergot derivatives
Action

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Block alpha-andrenergic and serotonin receptor sites in teh brain to cause cranial vaso constriction

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Ergot derivatives
Indications

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Prevention of abortion adn migraine or vascular headaches

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Ergot derivatives
Pharmacokinetics

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Absorbed by many routes
15-30 minute onset
Liver metabolizm
Bile excretion
Breast milk crossing

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Ergot derivatives
Contraindications

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Known allergy
Pregnancy and lactation
CAD
HTN
PVD

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Ergot derivatives
Cautions

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Pruritus
Malnutrition

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Ergot derivatives
Adverse reactions

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Numbness
Tingling of extremities
Muscel pain
Pulselessness
Weakness
Chest pain
Arrhythnias
Nausea
Vomiting
Diarrhea

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Ergot derivitives
Drug-Drug interactions

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Beta blockers-blocks coronary B receptors
Causes vasoconstriction of lungs

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Triptans
Actions

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Bind to selective serotonin receptor sites to cause cranial vasoconstricion

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Triptans
Indications

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Treatment of acute migraines
Not used for prevention of migranes

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Triptans
Pharmacokinetics

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Absorbed from many sites
Liver metabolism
Urine excretion
Placenta and breast milk crossing

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Triptans
Contraindications

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Known allergy
CAD, pregnancy

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Triptans
Cautions

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In the elderly; risk of CAD and lactation

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Triptans
Adverse reactions

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Numbness, tingling, burning sensation, feeling of coldness, weakness, dysphagia, blood pressure alterations

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Triptans
Drug-Drug interactions

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Ergot containing drugs
MAO's

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Triptan
Prototype

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Sumatriptan
Treatment of acute migraine; treatment of cluster headaches

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Ergot
Prototype

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Ergotamine
Prevention or abortion of vascular headaches