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PHARMACOLOGY REVIEW

PHARMACOLOGY REVIEW. LAST BLOCK. OPIOD. MAINLY OBTAINED FROM OPIUM POPPY. ACT BY BINDING TO SPECIFIC OPIOID RECEPTORS IN THE CNS. MAINLY USED FOR RELIEVING INTENSE PAIN. EUPHORIC PROPERTIES ANTAGONISTS IMPORTANT IN OVERDOSE. OPIOID RECEPTORS. 4 TYPES Mu ( µ ) Kappa ( к )

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PHARMACOLOGY REVIEW

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  1. PHARMACOLOGY REVIEW LAST BLOCK

  2. OPIOD • MAINLY OBTAINED FROM OPIUM POPPY. • ACT BY BINDING TO SPECIFIC OPIOID RECEPTORS IN THE CNS. • MAINLY USED FOR RELIEVING INTENSE PAIN. • EUPHORIC PROPERTIES • ANTAGONISTS IMPORTANT IN OVERDOSE.

  3. OPIOID RECEPTORS 4 TYPES • Mu ( µ ) • Kappa ( к ) • Delta ( δ ) • Sigma ( σ )

  4. Strong Agonists • Morphine • Fentanyl • Heroin • Meperidine • Methadone • Sufentanil

  5. Moderate Agonists • Codeine • Propoxyphene

  6. Mixed agonist - antagonist • Buprenorphine • Pentazocine

  7. MORPHINE • Main agonist actions on Mu, and also for Kappa and Sigma receptors ACTIONS: - Analgesia – relief of pain without loss of consciousness. - Euphoria - Causes Respiration Depression (This is the most common cause of death in acute opioid overdose)

  8. - Depression of cough reflex • MIOSIS – PINPOINT PUPIL. • Stimulation of the edingerwestphal nucleus of oculomotor nerve which causes parasympathetic stimulation of the eye. • Emesis.—stimulates chemoreceptor trigger zone (CTZ) in area postrema • - GIT : ↓ motility, relieves diarrhea and dysentery - CVS : high doses cause hypotension and bradycardia

  9. METHADONE • MECH: More on Mu receptors • Equal potency to Morphine, but less euphoric and longer duration of action. Actions: • Mostly same as morphine. • Route : oral • Met: Liver • Exe: Urine USES : • Analgesia • Addicts of heroin and morphine – for withdrawal . SE: • Less severe than morphine.

  10. HEROIN • 2-3 times more potent than morphine. • More euphoria • No therapeutic uses • Addiction

  11. PROPOXYPHENE • Derivative of Methadone • Analgesic for mild to moderate pain • Sometimes used in combination with aspirin or acetaminophen - ↑ analgesia • Also has antitussive action (used for cough)

  12. CODEINE • Good antitussive, • Less analgesic than morphine • Causes euphoria • Sedation • Addiction • So, many of the newer cough medications do not contain codeine • It has been replaced by dextrometharphan

  13. FENTANYL • AROUND 100 TIMES MORE POWERFUL ANALGESIC THAN MORPHINE, SO USED during ANESTHESIA • Rapid action and short duration of action. • Main action is on Mu, and also on kappa sigma receptors.

  14. NALOXONE • OPIOID ANTAGONIST • Rapidly reverse the effects of opioids, which can increase withdrawal symptoms • Reverse the coma and resp depression of opioid overdose. • IV route – In 30 sec shows significant changes in resp depression and coma. • Precipitates the withdrawal symptoms in morphine and heroin abusers.

  15. NALTREXONE • SAME AS NALOXONE • Longer duration of action than naloxone • Oral route • Used in opiate dependence maintainance programs.

  16. DEPRESSION • INTENSE FEELINGS OF SADNESS • HOPELESSNESS • DESPAIR • INABILITY TO EXPERIENCE PLEASURE IN USUAL ACTIVITIES.. • Weight loss/weight gain • Changes in sleep pattern • Recurrent thoughts of death • Suicidal tendencies

  17. MANIA • OPPOSITE BEHAVIOR • ENTHUSIASM • RAPID THOUGHT AND SPEECH . • IMPAIRED JUDGEMENT.

  18. Tricyclic antidepressants (TCAs) • Amitriptyline • Imipramine - NOREPINEPHRINE • Desipramine • Doxepin • Clomipramine - SEROTONIN • Nortriptyline • Protriptyline • Maprotiline – Second generation • Amoxapine -- Second generation

  19. MODE OF ACTION • These drugs are thought to increase levels of norepinephrine and serotonin in the synaptic cleft by blocking neuronal reuptake. • They also block histamine, cholinergic and alpha-adrenergic receptors. Which accounts for a large proportion of their side effects

  20. Actions • Elevate mood • Improve mental alertness • ↑ physical activity • More than 2 weeks need..

  21. Clinical indications for tricyclics • Mood disorders • Panic disorder • Generalized anxiety disorder • Posttraumatic stress disorder(clomipramine) • Pain disorders • Enuresis in children(imipramine)

  22. Serotonin- specific reuptake inhibitors (SSRIS) • FLUOXETINE (PROZAC) • SERTRALINE (ZOLOFT) • PAROXETINE( PAXIL) • FLUVOXAMINE (LUVOX)

  23. Action • New group • Selectively inhibit serotonin reuptake. • Fewer anticholinergic and lower cardiac toxicity. • USES: endogenous depression • obsessive-compulsive disorder • obesity • bulimia nervosa – (Fluoxetine)

  24. EPILEPSY PRIMARY or IDIOPATHIC SECONDARY KNOWN CAUSES: • HEAD INJURY • TUMORS • MENINGITIS • HYPOGLYCEMIA • DRUG WITH DRAWAL

  25. The two main categories of seizures include • Partial seizures – no loss of consciousness • and • Generalized seizures – loss of consciousness • A partial seizure can evolve to a generalized seizure.

  26. Simple Partial • These produce symptoms associated with the area of abnormal neural activity in the brain confined to single locus: • The electrical discharge does not spread • Can occur at any age • motor signs, sensory symptoms, autonomic signs and symptoms • There is no impairment of consciousness in simple partial seizures.

  27. Complex Partial • Impairment of consciousness, characteristic of complex partial seizures (CPS) • results in the inability to respond to or carry out simple commands or to execute willed movement, and a lack of awareness of one’s surroundings and events. • Exhibit complex sensory hallucinations, mental distortion and motor dysfunction • Experience initial seizures before age of 20 yrs

  28. Generalized Seizures • At the onset, seizure activity occurs simultaneously in large areas of the brain, often in both hemispheres. • Begin locally and rapidly spread to both the hemispheres. • Loss of consciousness • Seizures can be convulsive or nonconvulsive. • The two most common types are tonic-clonic (grand mal) and • Absence (Petit mal).

  29. Status Epilepticus was defined as 30 minutes of continuous seizure activity or a series of seizures without return to full consciousness between the seizures

  30. CLASSIFICATION Seizures • PARTIAL / FOCAL • SIMPLE • COMPLEX • GENERALIZED • GRAND MAL ( tonic clonic) • PETIT MAL ( Absence) • MYOCLONIC • FEBRILE • STATUS EPILEPTICUS

  31. INHALED AGENTS HALOTHANE ENFLURANE ISOFLURANE SEVOFLURANE NITROUS OXIDE There potency is defined base on the concept of minimum alveolar concentration ( MAC)

  32. Definition • Elevation of arterial blood pressure above 140/90 mm Hg. Can be caused by: • - idiopathic process (primary or essential hypertension) • an underlying disease process (secondary hypertension) • Renal artery stenosis • Hyperaldosteronism • pheochromocytoma

  33. ANTI-HYPERTENSIVE DRUG CLASSES • Diuretics • Beta blockers • Vasodilators • Calcium Channel Blockers • Angiotensin Converting Enzyme (ACE) Inhibitor • Alpha blockers

  34. ACE INHIBITORS • ENALAPRIL • CAPTOPRIL • LISINOPRIL • QUINAPRIL • FOSINOPRIL • BENAZEPRIL • MOEXIPRIL

  35. USES • HTN • CHF • POST MI • Considered best drugs for HTN with DM.

  36. VASODILATORS • HYDRALAZINE • MINOXIDIL

  37. USES HTN, CHF. SE: whose main side effect is a lupus-like syndrome SLE NAUSEA VOMITING HEADACHE FLUID RETENTION ARRHYTHMIA ANGINA HYDRALAZINE

  38. MINOXIDIL SE: • SODIUM AND WATER RETENTION • VOLUME OVERLOAD • LEADING TO EDEMA & CHF • USED FOR TREATING REFRACTORY HTN • HYPERTRICHOSIS • For baldness

  39. DRUGS • ORGANIC NITRATES • BETA BLOCKERS • CALCIUM CHANNEL BLOCKERS

  40. Therapeutic uses • Acute angina attacks- use the sublingual form of nitroglycerin because the onset of action in seconds to minutes • Prevention of attacks- use the oral or transdermal form of nitroglycerin

  41. SIDE EFFECTS • MC: Headache The most common side effect of nitrates is headache. For most people, headaches subside after a few days • Dizziness, weakness due to postural hypotension. • Drug rash, especially with Pentaerythritol tetra nitrate.

  42. CALCIUM CHANNEL BLOCKERS • MECH –Inhibit the entrance of Ca into cardiac & smooth muscle cells of the coronary and systemic arterial beds. • GREATER EFFECT ON ARTERIOLES • DECREASES AFTER LOAD • DECRASES OXY. DEMAND

  43. USES • VARIANT ANGINA OR PRINZMENTAL’S ANGINA – DUE TO VASOSPASM • EXERTIONAL ANGINA • RAYNAUDS DISEASE

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