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Opioids(analgesic)

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alex0624's version from 2016-06-27 21:31

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opioid antagonistNaloxene(short acting) and Naltroxene(Long acting)
Mixed agonist-antagonis(partial agonist) opioidBuprenorphine, nalbuphine and pentazocine
Strong agonist opioidsMorphine, Methadone, Mepiridine, Fentanyl
Mild to moderate opioidscodiene, oxycodone, hydrocodone
G-Protein couple receptors(decrease cAMP).--> Mu receptor type--> Supraspinal and spinal analgesia; sedation; inhibition of respiration; solwed GI transit;modulation of hormone and NT releaseOpiods receptors
Opioids at presynapticInhibition of adenylate cyclase --->decrease cAMP--> decrease kinase activity -->inhibit the release of NT ACh, NE, 5-HT, glutamate, and substance P.
Opioids at post synaptic increase K+ currents → to hyperpolarization & ↓ firing
are contraindicative in head injuryOpioids
Analgesia, respiratory depresion, increase intracranial pressure, nausea, miosis(exept miperidine)Opiods CNS effects
Opioid that casuse heart tachycardiaMiperidine
Constipation by decreasing intestinal peristalsis and increase in muscle tone; increase billiary spinchter tone and pressure--> may cause biliary colicOpioids
DOC opioid in patients with biliary colicMeperidine
Contraindicative in head injury and billiary spasmOpiods
DOC for relief pain afeter MIMorphine(analgesic)
In high dose IV are often the major component of anesthesia for cardiac surgeryFentanyl and morphine.
Good for Acute pulmonary edema(venodilation and reduce afterload du to decrease in peripheral resistance)Opioids
Antitussive drugs(suppress cough at doses lower than needed for analgesiaCodiene and Dextromethorphan
antidiarrheal opioidsLoperamide(inmmodium) and Diphenoxylate
Opioid dependance(opioid Withdrawal)Methadone and buprenorphine
MOA: TOlerance to morphine(opioids in general). All effects****????by receptor uncoupling???
Dependance on opiates--> withdrawal effects seen. DOC?Buprenorphine and methadone
Withdrawal effects? higly depended on Half life.Chills, lacrimation, diarrhea, anxiety, myadriasis, hostility
Coma, miois and markerd respiratory depressionAcute opiate toxicity
For Opiate toxixity giveNaloxone(IV-1-4 hrs action)
MCC of death in opioid poisoninRespiratory depression
Opioid antagonist long durationNaltrexone(24 hrs)
subject physically dependent on opioids- use of antagonis may precipitate withdrawalAntagonist Precipitated withdrawal
Addictive CNS depression by other drugs combined with opioidsDrug interaction
Use of Meperidine with MAO inhibitors(TCA) can causeSerotonine syndrome
Weak SERT inhibitorMeperidine
Selective SERT inhibitorSSRI
Block SERT and NETTCA
Block reuptake of all monoaminesCocaine
Cause seizures at higher doses or patients with renal failure due to accumulation of its metabolite nomeeridineMeperidine
used in biliary colic(cause tachycardia)Meperidine
Converted to active form morphine by CP2D6Codiene
Codiene is converted to active morphine by te action ofCYP2D6
Failure to respone do codiene may be by CYP2D6 genetic variability
Most effective drugs for suppression of coughCodiene(orally)--> low doses
Suppress cough by depressing medullary cough center throug sigma receptorsDextromethophan
DOC for Cough supressionCodiene(morphine) or Dextromethorphan
COugh depressant that have little effect on CNSDextromethorphan
DOC for Neurlept analgesiaFentanyl + Droperidol
DOC for chronic malignant painFentanyl patches
Opioid more potent than morphineFentanyl
Used in Severe pain(terminal cancer), detoxification and mantainance of narcotic dependenceMethadone
Other name for heroine(opioid)Diacetylmorphine
Cause extreme euphoria, highly lipid soluble(crosses BB faster than morphine)IVHeroine(diacetylmorphine)
Drug approved for alcohol deaddiction(decrease craving for alcohol)Naltrexone
Pure opioid receptor antangonistNalmefene
1/3 as potent as morphinePentazocine
k agonist, m partial agonist (can precipitate withdrawl) Pentazocine
Effective orally; shorter duration and faster onset of action than morphinePentazocine
Strong k agonist, m antagonist (can precipitate withdrawl) Nalbuphine
Potent, long acting Partial m agonist, weak k , d anatgonist Use: opioid dependenceBuprenorphine
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