الرحماللهبسمالرحيمن

الله صدق

العظيم

Drugs which relieve pain be central action .

Certain drugs can relieve specific types of pain (not proper analgesic drugs) e.g., atropine in colics.

Peripheral analgesic include : physical protectives, local and surface anaesthetics , obtundants , astringents and counterirritants

No drug dependence

No euphoria or drowsiness.

Subcortical on thalamus

Relieve low intensity pain, e.g., headache , neuralgia, myalgia

Analgesic antipyretics

Addictive

Produce euphoria and stupor

Act cortical and subcortical .

Can relieve any type (except itching ).

Opioid (narcotic ) analgesic

Opioid actionsCNS: analgesia Respiratory and cough centre: depressionVomiting centre: Nausea Higher centres: Euphoria & dysphoria Bowel: relax. Uses: relief of pain ( ischemic-post operative- palliative Dirrhea (codeine)

Very old, very young . liver Very old, very young . liver disease and myxedema. disease and myxedema.

Acute abdominal pain (interfere Acute abdominal pain (interfere with diagnosis). with diagnosis).

Head injury , increased CSF Head injury , increased CSF pressure . pressure .

Respiratory disease. Respiratory disease. Delivery and lactation. Delivery and lactation. Biliary colic. Biliary colic. Acute alcoholism. Acute alcoholism. Epilepsy Epilepsy

PreparationsPreparations : Morphine HCI or : Morphine HCI or ulphate 10-15 mg S.C., I.M. or I.V. ulphate 10-15 mg S.C., I.M. or I.V.

Adverse effects:Adverse effects: Respiratory Respiratory depression, nausea , dizziness, depression, nausea , dizziness, mental clouding, dysphoria , mental clouding, dysphoria , pruritus, constipation , increased pruritus, constipation , increased biliary pressure, urine retention biliary pressure, urine retention and hypotension.and hypotension.

Analgesic and anti-inflammatory Analgesic and anti-inflammatory drugs especially drugs especially In chronic inflammation In chronic inflammation

Rheumatoid arthritis Rheumatoid arthritis Sever osteoarthritis Sever osteoarthritis Chronic back pain Chronic back pain

In acute injury with inflammation In acute injury with inflammation Dysmenorrhoea Dysmenorrhoea Pain from lytic bone metastases .Pain from lytic bone metastases .

Pyrazolone derivatives : rarely used due to bone marrow depression Adverse effects: GIT upset, salt and water retention, oedema, h7ypertension , bone marrow depression, liver and renal toxicity, skin rash, and bronchospasm. Indole derivatives : is potent Adverse effects: GIT disturbances , frontal headache , vertigo, confusion, psychosis , blood dyscrasias , liver and kidney toxicity, kin rash and asthma.

Classification Of NSAIDS

Sulindac: it is prodrug which is converted into active metabolite and ahs kess gastric irritation. Anthranilic acid derivatives: fenamates Central analgesic action (which is specific with mefenamic acid . Propionic acid derivatives (IBUPROFEN : Most safe Oxicams : Piroxicam (Feldene). It has enterohepatic cycle, so has long plasma half life

Gastric irritation , increased occult Gastric irritation , increased occult blood in stools. blood in stools. Hypersensitivity reaction: asthma, Hypersensitivity reaction: asthma, rash, …… rash, …… Idiosyncracy: In patient: with G-6-Idiosyncracy: In patient: with G-6-PD deficiency PD deficiency →haemolytic→haemolytic anaemia anaemia Prolonged use may lead to Prolonged use may lead to hypoprothrombinaemia. hypoprothrombinaemia.

Chronic use → Salicylism: Chronic use → Salicylism: Headache , mental confusion, Headache , mental confusion, vertigo, ringing in ears (tinnitus), vertigo, ringing in ears (tinnitus), Sweating , nausea, vomiting. Sweating , nausea, vomiting. Acute salicylate poisoning : Acute salicylate poisoning : Restlessness, tremors , Restlessness, tremors , convulsions vomiting , convulsions vomiting , dehydration, ↓ B.P., metabolic dehydration, ↓ B.P., metabolic acidosis (in children), respiratory acidosis (in children), respiratory alkalosis (in adults), hyperglycemia alkalosis (in adults), hyperglycemia , hyperpyrexia., hyperpyrexia.

1- 1- Epigastric distress, naused and Epigastric distress, naused and v0omiting ( # PGS in GIT) v0omiting ( # PGS in GIT) 2- 2- CVS & M.I.: with Cox-2 inhibitors CVS & M.I.: with Cox-2 inhibitors (rofecoxib )(rofecoxib )3- 3- Coagulation disorders (reversible )Coagulation disorders (reversible )4- 4- Renal toxicity (# Pgs). Renal toxicity (# Pgs). 5- 5- Hypersensitivity Hypersensitivity

N.B.N.B. Newer NSAIDS have lower Newer NSAIDS have lower incidence of gastric distribution but incidence of gastric distribution but higher incidence of renal damagehigher incidence of renal damage

Kinetics Kinetics

Major Major Minor Minor

Conjugate withConjugate with Toxic metaboliteToxic metabolite glucuronic and glucuronic and (N-acetyle Benzo quinone (N-acetyle Benzo quinone acid sulphate acid sulphate which is detoxificated which is detoxificated

by glutathione by glutathione

Adverse effects: Adverse effects: It is well tolerated at therapeutic doses. It is well tolerated at therapeutic doses.

Skin rash and drug fever, blood dyscrasias Skin rash and drug fever, blood dyscrasias (rare). (rare). Hepatic necrosis and renal tubular necrosis Hepatic necrosis and renal tubular necrosis and hypoglycemic coma. and hypoglycemic coma. Methemoglobinemia and haemolytic Methemoglobinemia and haemolytic anaemia (with Phenacetin ). anaemia (with Phenacetin ). Phenacetin may produce cyanosis , Phenacetin may produce cyanosis , respiratory and cardiac arrest in lethal respiratory and cardiac arrest in lethal doses.doses.