Opioid analgesics 3 Flashcards
Mention the symptoms of Abstinence syndrome?
- Generalized Muscle aching
- Dilated pupil, Diarrhea (DD)
- Insomnia, anxiety, restlessness
- Increased blood pressure and heart rate
Mention the treatment of addiction (Detoxification or Chronic toxicity or Physical dependence or adaptation) of morphine?
HGR GCO
- Hospitalization.
- Gradual Withdrawal of morphine.
- Replacement of morphine by another opioid as methadone, buprenorphine
- Gradual Withdrawal of methadone.
- Clonidine may be added to control sympathetic over activity
- Opioid antagonist (naltrexone) used in ex-abusers to block the effect of self- administrated opioids
Enumerate the adverse effect of morphine?
(ATC)
1. Acute morphine toxicity (Intoxication)
2. Tolerance due to down regulation of opiate receptors
3. Chronic toxicity (Physical dependence (addiction)/ adaptation / Detoxification
(NSRC)
4. Nausea, vomiting
5. Sedation, drowsiness, mental clouding, apathy
6. Respiratory depression, bronchospasm.
7. Convulsions
(CUB)
8. Constipation
9. Urine retention
10. Biliary colic
- Interfere with diagnosis of acute abdomen
- Interfere with diagnosis of head injury as it produce miosis
In Treatment of addiction of morphine, Replacement of morphine by another opioid as………………….and………………….
methadone, buprenorphine
Mention the Precautions of morphine use [contraindications] ?
- Asthmatic patients
- Age: Extremes of Age (infants, elderly)
- Adrenal insufficiency: morphine decrease ACTH
- Acute abdomen: morphine mask pain so interfere with diagnosis
- Head injury, interfere with diagnosis of head injury because Morphine cause miosis& mental disturbance
- Hepatic, renal dysfunction : lead to accumulation of morphine due to inadequate metabolism and excretion.
- Hypothyroidism (myxedema): morphine can induce myxedema coma
- Hypovolemia (reduced blood volume)
- At onset of Labor: morphine cross the placental barrier and cause asphyxia neonatorum
Analgesic effect of codeine related to demethylation of 10% codeine by……………into morphine
CYP 2D6
Mention the variation in analgesic and adverse responses to codeine on different types of metabolizers as a result of genetic polymorphism of CYP2D6?
1- Poor metabolizers: show non-significant analgesic effect of codeine.
2- Ultra rapid metabolizers: show exaggerated response to codeine due to enhanced metabolic conversion to
morphine that may end with respiratory depression and death.
Marked constipation induced by……….and…………
Codeine & Morphine
sympathetic over activity during morphine withdrawal controlled by………….and………….
Clonidine & Lofexidine
All the following is true about Codeine EXCEPT:
A. Weak opioid agonist
B. high affinity to opioid receptors
C. 10% of codeine demethylated by CYP 2D6 into morphine
D. powerful suppressant effect of cough center
B. high affinity to opioid receptors
Methyl morphine (less affinity to opioid receptors)
Active neuronal uptake of norepinephrine inhibited by………….&…………….
Tramadol {Analgesic}
Cocaine {local anesthetic}
Tramadol inhibit active neuronal uptake of monoamines (NE, 5HT) leading to……………..
Euphoria (Monoaminergic
activity, anti-depressant effect)
Side effects of Tramadol…………&………
seizure, physical dependence, addiction
Mention the drug that is more potent analgesic than morphine and highly lipid soluble, rapid onset and highly addictive?
Heroin
Mention the drug that have opioid like action on the gut, can not cross BBB and have an selective action on GIT => used for treatment of diarrhea?
Diphenoxylate and loperamide
