Meperidine (Demerol) Use : Commonly used in Labor

AE : Respiratory depression
Antimuscarinic (Mydriasis and dry mouth)
Anxiety → Psychosis due to toxic metabolite
Tremors &Convulsions Normeperidine
Tolerance &Dependence
DI : MAOi – convulsions and hyperthermia
Neuroleptics – enhanced depression
Cross tolerance w/ opioids
Methadone Use : Analgesia
Withdrawal of heroin and morphine abuse
Oxycodone Formulated with Aspirin or acetaminophen
&Hydrocodone(Morphine Ingestion of crushed tablet may lead to death
derivatives)
Fentanyl Use : Analgesia &Anesthesia
(Meperidine derivative) Ph Kinetics : Oral
100x more potent than Transmucosal (cancer)
morphine IV (Cardiac surgery)
Epidural (Post op &labor analgesia
AE : Muscle rigidity of abdomen and chest
Respiratory Depression and Miosis
Derivatives : SUFENTANIL ALFENTANIL RAMIFENTANIL
Heroin Produced by diacylation of morphine
(converted to morphine in Crosses the Blood brain barrier more rapidly
body; 3x more potent) Increased Euphoria

MODERATE AGONISTS
Codeine Action : Cough Suppression
(Synthesized from and Low analgesia
converted to Morphine) Euphoria
Sedation
Use : Antitussive &Analgesia
Adv : Lower abuse potential than morphine and less euphoria
Propoxyphene(Methadone AE : Nausea, Anorexia, Constipation
derivative) High doses: Respiratory depression, hallucination, convulsion
d isomer → Analgesic DI : synergism with acetaminophen
Lisomer → Antitussive alcohol &sedatives – severe CNS &respiratory depress.
&cardiotoxicity
Antidote: NALOXONE for sedation and respiratory depression
PARTIAL AGONISTS (MIXED AGONIST-ANTAGONIST)
Act as antagonist in the presence of strong agonists | Use: OPIOD DEPENDENCE
Act as agonist in the absence of antagonist | Use: ANALGESIC

Pentazocine AE (High dose) : Respiratory Depression

Constipation
Tachycardia
Dizziness
Nightmares
Hallucination
Tolerance and dependence
CI : Angina – Increase work of heart
Kidney disease – Decrease renal plasma flow
Buprenorphine Major use : Opioid detoxification
Preferred than Methodone due to less Respiratory depression,
Hypotension, Sedation
(IV) analgesia
(Sublingual) Opioid dependence
Nalbuphine &Butorphanol Use : limited role as analgesic
Adv : Less psychomimetic &CV effects than Pentazocine

Other Drugs:
Tramadol MOA : Binds to Opioid receptor &weakly inhibits reuptake of NE and 5HT
Use : Moderate to moderately severe pain
Adv : Less respiratory depression
DI : Antidepressants → Seizures

ANTAGONISTS
MOA : Blockade of Opioid receptors
Use : Reverse effects of agonists (for OD)
Precipitate w/d symptoms (dependence)

Naloxone Short duration but rapid (1 hour)

- Reverses respiratory depression without analgesia
Nalmefene Intermediate (16-20 hrs)
Naltrexone Long acting (48 hrs)
Used in combination with Clonidine &Buprenorphine
Also used for Chronic Alcoholism
AE: Hepatotoxic
Stages of Withdrawal
STAGE 1 (8 hours) STAGE 2 (8-24 hours) STAGE 3 (UP to 3 days)
Anxiety GI disturbance Hypertension
Drug craving Rhinorrhea Tachycardia
Anxiety Fever
Insomnia Chills
Mydriasis Tremors
Diaphoresis Seizures
Muscle pain
Diarrhoea

Degrees of Tolerance to Opioid Effects

High Moderate Minimal/None
Cough suppression Bradycardia Miosis
Urinary retention Constipation
Respiratory depression Convulsion
NV
Sedation
Analgesia
Mental clouding
Euphoria