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Card 1: Aspirin & Salicylates
Class: Non-Steroidal Anti-Inflammatory Drug (NSAID)
Mechanism of Action: Inhibits cyclooxygenase (COX) enzymes, leading to reduced prostaglandin synthesis.
Therapeutic Uses: Mild pain (Step 1 on WHO Pain Ladder).
High-Yield Side Effects & Toxins:
Peptic Ulcer & Bleeding: Gastrointestinal mucosal injury and prolonged bleeding time.
Reye's Syndrome: Severe brain and liver damage when given to children under 2 years old with a viral infection.
Salicylism (Toxicity): Features fever, bleeding, tinnitus/hearing loss, hallucinations, hyperventilation/increased respiratory rate, tachycardia, hypotension, convulsions, and coma.
Card 2: Morphine
Class: Natural Opioid Agonist
Mechanism of Action:
Agonist at (mu), (kappa), and (delta) G-protein coupled receptors.
Opens post-synaptic K^+ channels➡ hyperpolarization (decreases neuronal excitability).
Closes pre-synaptic voltage-gated Ca^{2+} channels➡decreases excitatory neurotransmitter release (e.g., Substance P in dorsal horn).
Pharmacological Effects:
CNS: Analgesia (spinal & supraspinal), euphoria, drowsiness, pin-point pupils (severe miosis via Edinger-Westphal nucleus stimulation), respiratory center depression, cough suppression, nausea/vomiting (via CTZ stimulation).
CVS & Smooth Muscle: Orthostatic hypotension (vasomotor center depression & histamine release), peripheral bronchospasm, sphincter contraction causing constipation, urinary retention, and biliary pressure increase.
Endocrine: Decreases LH, FSH, and ACTH levels \rightarrow loss of libido, impotence, and menstrual irregularities.
Therapeutic Uses: Severe pain (burns, trauma, post-op, terminal cancer), pre-anesthetic medication, epidural/intrathecal segmental analgesia, and relief of anxiety in acute myocardial infarction or severe internal bleeding.
Contraindications:
Obstetrics: Avoid during labor (causes fetal neonatal asphyxia due to immature blood-brain barrier).
Abdominal Pain: Contraindicated in acute undiagnosed abdomen and diagnosed biliary colic/renal colic (causes sphincter contraction).
Head Injury: Contraindicated due to increased intracranial pressure/respiratory depression.
Organ Failure: Severe hepatic or renal failure.
High-Yield Board Facts:
Non-Tolerated Side Effects: Patients develop tolerance to analgesia, euphoria, sedation, and respiratory depression, but NO tolerance develops to miosis and constipation.
Withdrawal: Autonomic hyperactivity (lacrimation, rhinorrhea, sweating, dilated pupils, diarrhea, hyperpyrexia) and muscle/joint aches.
Overdose Triad: Respiratory depression + Pin-point pupils + Coma (plus hypothermia & hypotension). Treat with Naloxone.
Card 3: Codeine
Class: Natural Opioid Agonist
Mechanism of Action: Low-potency \mu-receptor agonist. Prodrug that requires metabolic conversion (approx. 10%) into morphine for analgesic activity.
Therapeutic Uses: Mild to moderate pain, powerful selective cough suppressant (antitussive), and diarrhea treatment.
High-Yield Board Facts: Significantly lower potency, efficacy, addiction potential, and withdrawal severity compared to morphine.
Card 4: Meperidine (Pethidine)
Class: Synthetic Opioid Agonist
Mechanism of Action: Synthetic(kappa) agonist.
Therapeutic Uses:
Labor Analgesia: Preferred because it does not suppress fetal respiration like morphine.
Colic Pain: Indicated for severe renal and biliary colic because it acts as a smooth muscle relaxant.
High-Yield Board Facts:
Not used for cough or diarrhea.
Less potent than morphine but more potent than codeine.
Causes rapid dependence and short withdrawal symptoms.
Card 5: Tramadol
Class: Synthetic Codeine Analog / Dual-Action Analgesic
Mechanism of Action: Weak \mu-receptor agonist AND blocks reuptake of Norepinephrine (NE) and Serotonin (5-HT) in the CNS
Therapeutic Uses: Mild to moderate visceral pain (diagnostic procedures, injury, surgery).
Contraindications & High-Yield Toxicity:
SSRI Therapy: Strictly contraindicated with SSRIs due to the risk of triggering Serotonin Syndrome.
6.Fentanyl
Synthetic μ agonist, with 80 times higher analgesic effect & respiratory depression than morphine, used in anesthesia.
Because of high lipid solubility, it enters brain rapidly and produces peak analgesia in 5 min after i.v. injection.
The duration of action is short- 30–40 min
Transdermal fentanyl has become available for use in cancer/ terminal illness or other types of chronic pain for patients requiring opioid analgesia.
Transdermal fentanyl patches are approved in sustained pain.
Rectal administration
Oral transmucosal administration: Fentanyl in a dissolvable sugar- based lollipop or rapidly dissolving buccal tablet have been approved for the treatment of cancer pain Trans-nasal administration
7.Methadone
Slow tolerance & less physical dependence with mild withdrawal symptoms
Used for treatment of opioid abstinence (withdrawal) syndrome
Produces long QT syndrome: potentially fatal adverse effect OPIOID ANTAGONIST Naloxone
Pure opioid antagonist used to treat respiratory depression in opioid toxicity
Cause withdrawal symptoms in addicts CHRONIC PAIN: ROUTES OF ADMINISTRATION OF OPIATES
Spinal delivery: Administration of opioids into the epidural or intrathecal space
تجميعات
-A patient came into the ER with lacrimation, increased heart rate, sweating
and dilated pupils. Which drug is used to manage his condition?
A. Naloxon
B. Morphine
C. Opioid
D. Methadone
Answer: D
-.A 50 year old man is having sleep apnea and he wants to take an opioid for
his severe back pain. Which of the side effects will likely occur?
A. Respiratory depression
Answer: A
1. A pregnant woman in labour who previously had biliary colic. What analgesic should be given for her labour?
A. Meperidine
Answer: A
2. A patient came in the ER with lacrimation, increase heart rate, sweating and dilated pupils. Which drug is used to manage his condition?
A. Naloxone
B. Morphine
C. Opioid
D. Methadone
Answer: D
3. Which one of the following drugs is used during labor?
A. Methadone
B. Morphine
C. Meperidine
D. Opioid
Answer: C
4. Which one of the following is used during anesthesia?
A. Fentanyl
B. Tramadol
C. Meperidine
D. Opioid
Answer: A
5. A 20-year-old patient came to the ER with respiratory distress, pin-point pupil, hypothermia and hypotension. What’s the drug of choice to treat him?
A. Morphine
B. Meperidine
C. Codeine
D. Naloxone
Answer: D
الصيغة الاصلية:
Morphine poisoning antidote?
A. Naloxone
Answer: A
6. A 30-year-old woman is undergoing labour, Which of the following analgesic drugs is suitable for her?
A. Morphine
B. Codeine
C. Fentanyl
D. Meperidine
Answer: D
الصيغة الاصلية:
During labour an anesthetic drug is given
A. Meperidine
Answer: A