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INSULIN &OTHER GLUCOSE LOWERING DRUGS

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Diabetes Mellitus Heterogenous group of syndromes characterizes by elevated Blood Glucose level caused by relative or absolute deficiency of INSULIN. Pancreas is an Endogenous gland, produces Insulin, Glucagon, Somatastatin… Pancreas is also an exogenous gland produce digestive enzymes…β-cells produce insulin, α-cells Glucagon, δ-cells produce Somatostatin… Click and learn insulin conceptually Type-1 Diabetes Mellitus  young individual, Autoimmune destruction of β-cells, Pancreas fail to respond Glucose……..required Exogenous Insulin to avoid Catabolic state characterized by Hyperglycemia & Ketoacidosis….. Insulin deficiency symptoms Polydipsia, Polyphagia, Polyuria, weight loss Type-2 Diabetes Mellitus  by Genetic factor, obesity, aging, peripheral insulin resistance older patients...β-cells become resistance to insulin...infection lead to Amputation Gestational Diabetes Mellitus  abnormality ofglucose in first term of Pregnancy Insulin & its analogue MOA insu...

Pituitary and thyroid gland - Drugs acting on pituitary and thyroid

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 Adrenocorticotropin Hormone ACTH (Coticopropin) Require for melanin production…used in west syndrome…target organ Adrenal cortex.. Side effects= osteoporosis, peripheral edema, hypokalemia Somatotropin (Growth Hormone) In Anterior pituitary… Secretion of this hormone inhbited by Somatostatin… Acromegaly increase growth due to high GH ... used in Prader-Wili Syndome, AIDS west syndrome,short bowel syndrome…used in Paeds with Closed Epiphyses Antiaging hormone = called antiaging hormone bcz it increase Lean body mass, bone density, skin thickness, adipose tissue mass decreases…..abuse by some Athletes half life of GH 25min , produce IGF-I(Somatomedin C) produce action like GH S.E= Pt. develop Diabetes, avoid in pt. with inresed intracranial pressure, Diabetes Retinopathy, Obese pt. with prader-willi syndrome Somatostatin (Growth hormone –inhbiting hormone) Bind to SSTR2 & SSTR5….suppresGH & Thyroid stimulating hormone…found in intestine & pancreas…obtain from Hyp...

DIURETICS - CARDIOVASCULAR DRUGS ( PART 7/7) LIPINCOTT AND KADZUNG REVIEW CHAPTES

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 Thiazide Diuretics Sulphonamide derivative..related in structure to Carbonic Anhydrase….partly depend on renal PG synthesis Act on DISTAL CONVULATED TUBULE….called Ceiling Diuretics b/c increase in dose above normal dose not increase Diuretic response MOA= Act on distal tubules...inhibit Na+/CI- Cotransporter…decrease Reabsorption of Na+….increased Excretion of Na+ & CI-..Loss of K+..Loss of Mg++..decreased excretion of Ca++…reduced peripheral Vascular Resistance T.E= used in Hypertension, HF (decrease extracellular volume), Hypercalciuria,Diabetes Insipidus…… excreted thhroughorganic acid secretary sys of kidney S.E= Hypokalemia, Hyonatremia, HyperUricemia (by decreasing excretion of uricacid from organic acid secretary sys), Volume depletion, Hypercalcemia, Hyperglycemia,Hyperlipidemia, Hypersensitivity Loop Diuretics Act on ASCENDING LOOP OF HENLE….high Efficacy…Ethacrynic acid has Steeper Dose Response Curve….Bumetanide more potent MOA= inhbit Na+/K+/2CI-Cotransport in ...

HYPERLIPIDEMIA - CARDIOVASCULAR DRUG (PART 6B / 7) | PHARMACOLOGY REVIEW

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 HMG CoA Reductase Inhibitors (Statins)  3-Hydroxy-3-MethylGlutryl-Coenzyme A reductase inhibitors lower LDL Cholesterol level..Rate limiting step Cholesterol synthesis MOA =Statin inhibit HMG Co A reductase ...which convert HMG CoA into Mevalonic Acid which convert into Cholesterol…decrease conc. Of Cholesterol within cell Low intracellular Cholesterol stimulate synthesis of LDL receptor…Increased LDL receptor promote uptake of LDL from blood Low intracellular Cholesterol decrease Secretion of VLDL Increase plasma HDL level T.E= All types of Hyperlipidemia…..Familial Hypercholeserolemia lack LDL receptor so benefit less S.E= myopathies, rhabdomylysis, increase LFT, t1/2 1.5-2hr...Lova & Simva prodrug Contraindicated in pregnancy & lactation, teenage & children… Niacin (Nicotinic acid)  reduce LDL(Bad cholesterol), increase HDL(good  cholesterol ) MOA =inhibit Lipolysis in Adipose tissue…decrease level of Free Fatty Acids..liver use these Free Fatty A...

ANTI-COAGULANTS - cardiovascular drugs (part 6A/7)

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Inhibit the co-agulation by inhibiting Thrombin or Vit K anatagonists Heparin =Glycosaminoglycan…have negative charge…Acidic due to Sulphate & Carboxylicacid group….high moleculat weight…extracted from Porcine Intestinal Mucosa Complexed with Histamine in Mast cells…Low molecular weigh heparin(LMWH)<6000 MOA =interact with AntiThrombin lll…speed up process of anti-coagulant ofn Antithrombin LMWH complex with Antithrombin & Inactivate Factor Xa…Prothrombin not convert into Thrombin…no formation of fibrin T.E= used in Deep Vein Thrombosis…pulmonary embolism...Prophylactically in Pt. to avoid Postoperative thrombus during Elective surgery Do not cross placenta...used in Pregnant women with Prosthetic heart valve P.K =i.v administer...I/M inj leads to Hematoma formation…1-2hr t1/2…4hr of LMWH.. Titrate the infusion forr7-10 days so aPTT (activated Partial Thromboplastin time) b/w 1.5-2.5…. .taken up by Monocyte/Macrophage Sys for metabolismS.E= Hemorrhage...used Protamine sulph...

Blood drugs- Cardiovascular drugs ( Chapter 5/7) | Lipincott review

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  Thrombus= A clot that adheres to vessel wall Embolus= intravascular clot that floats in the blood Platelet aggregation inhibitor Platelet Aggregation =Stimulation of Platelets by Thrombin, Collagen and ADP… Activation of Phospholipase..liberate Arachidonic acid..Arachidonic acid convert into Prostaglandin H2(PG) by COX-1….PG H2 convert into TX A2 ..cause aggregation Fibrinogen attach GP IIb/IIIa receptor..cross-linking..aggregation of platelets Aspirin= inhibit COX1 by irreversible Acetylation of Serine…Arachidonic acid not convert into TX A2…..inhibit aggregation Also inhibit TX A2 Synthetase…activate Prostacyclin...furthur inhibition of aggregation… Ibuprofen anatagonize platelet inhibition by Aspirin Aspirin is only NSAID that irreversibly exhibit antithrombotic property…81mg of Aspirin known as “Baby Aspirin”….S.E; bleeding time prolong Clopidogrel, Ticlopidine, Prasugrul= MOA= irreversibly inhibit binding of ADP to GP IIb/IIIa…inhibit activation of receptor…inhibit...

Hypertension And use of Antihypertensive (chapter 4/7)

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  Hypertension= sustained systolic B.P of >140mmHg or a sustained Diastolic B.P of >90mmHg  DASH= Dietary Approach to Stop Hypertension…include fruit, vegetables, low fat dairy products, low in fat cholesterol & sodium Renin inhibitors Aliskerin= directly inhibit RENIN….contraindicated in Pregnancy…cause cough, angioedema, hyperkalemia, diarrhea   Centrally acting adrenergic drugs Clonidine=α2-agonist...Centrally decrease Adrenergic outflow …decrease sympathetic firing rate &noeepinephrine release….  Useful in Hypertension complicated by renal  disease…..cause Na+ water retention... rebound hypertension occur     α 2-Methyldopa = converted into MethylNorepinephrine….. Centrally decrease Adrenergic outflow ….decrease total peripheral resistance& B.P … treat Hypertenson   with Renal Impairment……cause sedation, dizziness...can be used in pregnancy Vasodilators MOA=direct smooth muscle relaxant…vasodilation....