Opioids Flashcards
Morphine
Mu agonist
May be good foor arythmias due to anxiolytic effect
Adjuvant therapy for pulmonary edema- decreases air hunger.
Cancer pain at step 3
For chronic pain but contraindicated in fibromyalgia
Hydromorphine
Lower bioavailability (%20)
More potent than morphine 7-8 times.
Oxycodone
Strong mu agonist
Cyp2d6 metabolite= turned into active comp.
Good bioavailability, almost twice stronger than morphine
Oxycodone+ naloxone combo can be used for analgesic effect without constipation
Pitiramide
Strong agonist. Less side effects than morphine but sedation is more often
Tapentadol
Mu agonist+ NET
Less opioid like side effects
Fentanyl
Much potent than morphine
Transdermal- changed every 3 days
Fentanly+ antipsychotics= consciouss surgery
Methadone
Strong opioid agonist with NET-SERT effect.
QT prolongation
LOPEROMİDE
Strong opioid agonist
Penetrated bbb in a very limited ratio
For treatment of diarrhea
Codeine
Weak opioid agonist- turned into its active component by cyp2d6
Tramadol
Turned into its active component via cyp2d6 metabolism
28) Explain the autonomous effects of morphine. What are the most important differences with tramadol?
a. Morphine is a potent mu opioid agonist that will increase pain threshold levels and have analgesic and sedative effects. It will also decrease gastric emptying, depress the respiratory system (which can be lethal), and reduce the motility of contractile organs.
b. Tramadol is a racemic mixture of a weak mu opioid agonist and norepi/serotonin reuptake inhibitor. It is much more bioavailable than morphine and can be taken orally. Its metabolite following first pass metabolism has even higher analgesic activity than tramadol itself. Like morphine, it is an analgesic but will have less side effects due to its less potent mu opioid activity. Both can cause nausea and vomiting but tramadol will have less constipation. Tramadol also has a higher threshold for tolerance and withdrawal symptoms will be less pronounced.
Cyp2d6 inhibitors?
Fluoxetine
Propranolol
Omeprazole(PPI)
SELEGLİNE(mao-i for parkinsons)
Venflaxine ( sert-net- snri)
Bupropion( net-dat antidepressant- for smoking cessation)
Duloxetine ( sert net- snri)
Ritonavit(hiv treatment)
Cocaine
Is codeine contraindicated in gastric ulcer?
No, codeine can be used as an analgesic for patients with gastric ulcers, as chronic paracetamol use for chronic ulcer patients can worsen their condition. Codeine and paracetamol combined can synergistically help with gastric ulcer pain, but again there is risks.
i. Codeine = delayed gastric emptying prolonged acid exposure in the stomach which is not ideal for patient with peptic ulcer history
ii. Paracetamol = COX1 inhibition that has GI implications due to inhibited prostaglandin synthesis bad for peptic ulcer patient
Buphrenorphine
Mixed agonist/ antagonist effect. Partial mu opioid agonist
Can be combined with other opioids.
Reduces cravings for other opioids and it also has weaker effects
combines with morphine to treat cancer pain to potentiate analgesic without as much of a risk of respiratory depression; prominent first pass and cannot be given orally
For all 3 receptors
Buphrenorphine + phenobarbital
Due to their effects on the central nervous system, using buprenorphine together with PHENobarbital may occasionally lead to serious side effects such as respiratory distress, coma, or even death. In addition, PHENobarbital may reduce the blood levels of buprenorphine, which may make the medication less effective.
Also it may do the same with naloxone
Also with metadone, it risks delayed opioid withdrawal.
