OPIOIDS - Opiate Education: Key Points for the Pharmacist

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 Pain =unpleasant sensation acute or chronic consequence of neurochemical processin

the peripheral and CNS.

Opioids are natural or synthetic compounds that prodce Morphine-like effect

Opioids Receptors= Protein receptors in CNS ,periphery and GIT..μ(mu), k(kappa),

δ(delta) ..

Opioid Pharmacology Three major types of opioid receptors are involved in analgesia: mu, delta, and kappa receptors. Activation of mu receptors produces analgesia, sedation, euphoria, respiratory depression, constipation, and physical dependence.


Morphine=Prototype, high affinity for μ receptor

MOA= inhibit Adenylyl cyclase..increase K+ ion ..hyperpolarization..decrease Ca++influx

..Morphine act at k receptor in spinal cord & decrease Substance P..modulate pain

ACTIONS=Analgesic by rising pain threshold in spinal cord & altering pain perception in

brain...Euphoria..Respiratory Depression..Depression of Cough reflexes..Miosis(pin

point pupil)....Emesis by stimulating CTZ..decrease GIT movement..Dilate CSF so

contra in Brain injury..Histamine release..increase Growth hormone.. Prolong Labor

T.E= induce Sleep...treatment of Diarrhea...Relief of Cough...treatment of Acute

Pulmonary Edema

P.K=linear P.K..First pass met..Morphine-6-Glucuronide potent analgesic..

S.E=Respiratory depression..increase intracranial pressure in head injury...urinary

retention in BPH..Tolerance & physical dependence..contra in pregnancy

Constipation; treated by stool softener Docusate & laxative Senna

Meperidine=Synthetic opioid..for Acute pain..actions same to Morphine..dont cause

Pin Point Pupil..but causes dilation of pupil due to anticholinergic effect..

Not used in treatment of cough & diarrhea..neurotoxic properties..

S.E=Hypotension, Mydriasis, Hyperactive reflexes, dry mouth,blurred vision,

Methadone= analgesic coparable to morphine..not induce Euphoria..

MOA= anatagonist of NMDA receptor..also mediated by μ receptor..

T.E= in Neurogenic pain..used in controlled withdrawl from Heroin & Morphine..

S.E=Torse-de-point..highly lipophilic..show genetic polymorphism

Fentanyl=100 fold analgesic property of Morphine..short duration 15-30min..used in

Anesthesia...for analgesia postoperatively & during labor...in cancer patient with

breakthrough pain..

Transdermal patch can cause death due to Hypoventilation, ..causes meiosis

Heroin=DiacetylMorphine..not occurnaturally..cross B.B.B..not in medical use

Oxycodone & Oxymorphone= Semisynthetic derivative of Morphine..formulated with

Aspirin & Acetaminophen.. Analgesic 2 times to Morphine..immediate & exteneded

release tab

Opioids are a group of analgesic agents commonly used in clinical practice. There are three classical opioid receptors (DOP, KOP and MOP), while the novel NOP receptor is considered to be a non-opioid branch of the opioid receptor family. Opioids can act at these receptors as agonists, antagonists or partial agonists.


Hydromorphine & Hydrocodone= Hydromorphine prefer over Morphine in renal

dysfunction..8-10 time more potent

MODERATE/LOW AGONIST

Codeine= convert into Morphine by CYP2D6..Antitussive effects due to Codeine..

30%more potent than Morphine...

MIXED AGONIST-ANTAGONIST & PARTIAL AGONISTS

Drugs stimulate one receptor but block another

Pentazocine=agonist on k receptor..weak antagonist at μ & δ...analgesic..increase

pulmonary arterial pressure

Buprenorphine= partial agonist at μ receptor..use in Opiate Detoxification..

Nalbuphine & Butorphanol= in Chronic pain..Psychotomimetics effects

OTHER ANALGESICS

Tramadol= μ receptor activation...block reuptake of Serotonin & Norepinephrine....

Anaphylactoid reaction reported...interaction with MOAI, Tricyclic depressents

Tapentadol= μ receptor activation...block reuptake of Norepinephrine..

ANTAGONISTS

Naloxone= competitive antagonist of μ, k, δ receptors...reverse coma & Respiratory

depression...within 30sec of i.v inj...no pharmacological effect..

Naltrexone= longer duration of action than Nalaxone...combined with Clonidine for rapid Opioid detoxification

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