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P h a r m a c o l o g yG e n e r a l p h a r m a c o l o g yStudy today, save lives tomorrow. | Every page you read brings you closer to becoming a doctor. | Small daily progress leads to great medical achievements. | Knowledge is the first step toward healing. | Never stop learning because medicine never stops evolving. | Your future as a doctor is built by what you learn today. | Dream big, study hard, heal humanity. | Every page brings you one step closer to your white coat. | Discipline builds the doctor that motivation only dreams of. | Every hour of study is an investment in your future patients. | Stay focused. Stay determined. Stay committed to medicine. | Behind every great doctor is a history of hard work. | Learn something new every day; your future patients will thank you. | Great doctors are built through years of learning. | Believe in yourself, trust the process, and keep studying. | The more you learn, the better you serve. | Success in medicine begins with preparation. | Every medical book is a step toward saving lives. | Your only competition is yesterday's version of yourself. | Study with purpose. Practice with confidence. Heal with compassion. | Don't give up. Every chapter brings you closer to your dream. | Medical excellence is the result of consistent effort. | Every .lecture is a step toward becoming the doctor you aspire to be. | Focus on progress, not perfection. | Today's student, tomorrow's healerM o d u l e | F o u n d a t i o n 2 P h a r m a c o l o g yMS1M e d i c a l S t u d e n t sF i r s t - y e a rD e f i n i t i o n s1ILO Important Definitions in pharmacology. Pharmacokinetics. pKa of drug. Bioavailability. Factors affect bioavailability. 1st pass metabolism. Volume of distribution (Vd). Significance of Vd. Factors affecting the distribution of drugs. Redistribution of drugs. Passage of drugs across barriers.P h a r m a c o l o g yD r u g sA bs o r pt i o n a n d D i s t r i b u t i o n L e c t u r e A b s o r p t i o n a n d D i s t r i b u t i o n 1M e 3 w a n 0 1 Pharmacology: is The science that deals with the study of drugs.Drugs: Chemical substances stimulate or inhibit an existing cell function (but do not create a new function in the cell). They are used in diagnosis, treatment & prevention of disease or in prevention of pregnancy.
P h a r m a c o l o g yG e n e r a l p h a r m a c o l o g yStudy today, save lives tomorrow. | Every page you read brings you closer to becoming a doctor. | Small daily progress leads to great medical achievements. | Knowledge is the first step toward healing. | Never stop learning because medicine never stops evolving. | Your future as a doctor is built by what you learn today. | Dream big, study hard, heal humanity. | Every page brings you one step closer to your white coat. | Discipline builds the doctor that motivation only dreams of. | Every hour of study is an investment in your future patients. | Stay focused. Stay determined. Stay committed to medicine. | Behind every great doctor is a history of hard work. | Learn something new every day; your future patients will thank you. | Great doctors are built through years of learning. | Believe in yourself, trust the process, and keep studying. | The more you learn, the better you serve. | Success in medicine begins with preparation. | Every medical book is a step toward saving lives. | Your only competition is yesterday's version of yourself. | Study with purpose. Practice with confidence. Heal with compassion. | Don't give up. Every chapter brings you closer to your dream. | Medical excellence is the result of consistent effort. | Every .lecture is a step toward becoming the doctor you aspire to be. | Focus on progress, not perfection. | Today's student, tomorrow's healerM o d u l e | F o u n d a t i o n 2 P h a r m a c o l o g yMS1M e d i c a l S t u d e n t sF i r s t - y e a rWhat the drug does to the body. It studies the mechanism of drug action & pharmacological actions.A Absorption From the site of administration into the systemic circulation Distribution From the bloodstream to intracellular and interstitial fluids.DM Metabolism The biochemical process by which the body chemically modifies drugs to make them easier to Excretion The drug and its metabolites are excreted from the body in urine, bile or feces.EWhat the body does to the drug or movement of the drug in the body. (ADME) L e c t u r eC y p e r s e c u r i t y 2M e 3 w a n 0 1S u b d i v i s i o n s o f P h a r m a c o l o g yP h a r m a c o k i n e t i c Pharmacodynamics Pharmacotherapeutics Pharmacovigilance Study the selection and use of drugs for diagnosis, treatment & prevention of disease. Science and activities relating to the detection, assessment, understanding, and prevention of adverse effects of drugs.M C QP h a r m a co k i n et i c0 1 Pharmacokinetics describes what the body does to the drug through ADME.ADMEAbsorption, Distribution, Metabolism, Excretion)
P h a r m a c o l o g yG e n e r a l p h a r m a c o l o g yStudy today, save lives tomorrow. | Every page you read brings you closer to becoming a doctor. | Small daily progress leads to great medical achievements. | Knowledge is the first step toward healing. | Never stop learning because medicine never stops evolving. | Your future as a doctor is built by what you learn today. | Dream big, study hard, heal humanity. | Every page brings you one step closer to your white coat. | Discipline builds the doctor that motivation only dreams of. | Every hour of study is an investment in your future patients. | Stay focused. Stay determined. Stay committed to medicine. | Behind every great doctor is a history of hard work. | Learn something new every day; your future patients will thank you. | Great doctors are built through years of learning. | Believe in yourself, trust the process, and keep studying. | The more you learn, the better you serve. | Success in medicine begins with preparation. | Every medical book is a step toward saving lives. | Your only competition is yesterday's version of yourself. | Study with purpose. Practice with confidence. Heal with compassion. | Don't give up. Every chapter brings you closer to your dream. | Medical excellence is the result of consistent effort. | Every .lecture is a step toward becoming the doctor you aspire to be. | Focus on progress, not perfection. | Today's student, tomorrow's healerM o d u l e | F o u n d a t i o n 2 P h a r m a c o l o g yMS1M e d i c a l S t u d e n t sF i r s t - y e a r1Simple diffusion (Passive diffusion – lipide diffusion )234Filtration (aqueous diffusion) (Diffusion through aqueous channel).L e c t u r eC y p e r s e c u r i t y 3M e 3 w a n 0 1A b s o r p t i o n0 1DefiiÜi It is the transport of the drug from the site of administration to the systemic circulation.Q u e s t i o n . . . ? How can drugs cross cell membrane?A Facilitated diffusion. Active transport D r u g p a s s a g e a c r o s s c e l l m e m b r a n e sM C Q
P h a r m a c o l o g yG e n e r a l p h a r m a c o l o g yStudy today, save lives tomorrow. | Every page you read brings you closer to becoming a doctor. | Small daily progress leads to great medical achievements. | Knowledge is the first step toward healing. | Never stop learning because medicine never stops evolving. | Your future as a doctor is built by what you learn today. | Dream big, study hard, heal humanity. | Every page brings you one step closer to your white coat. | Discipline builds the doctor that motivation only dreams of. | Every hour of study is an investment in your future patients. | Stay focused. Stay determined. Stay committed to medicine. | Behind every great doctor is a history of hard work. | Learn something new every day; your future patients will thank you. | Great doctors are built through years of learning. | Believe in yourself, trust the process, and keep studying. | The more you learn, the better you serve. | Success in medicine begins with preparation. | Every medical book is a step toward saving lives. | Your only competition is yesterday's version of yourself. | Study with purpose. Practice with confidence. Heal with compassion. | Don't give up. Every chapter brings you closer to your dream. | Medical excellence is the result of consistent effort. | Every .lecture is a step toward becoming the doctor you aspire to be. | Focus on progress, not perfection. | Today's student, tomorrow's healerM o d u l e | F o u n d a t i o n 2 P h a r m a c o l o g yMS1M e d i c a l S t u d e n t sF i r s t - y e a rSimple diffusion (lipid diffusion): is the chief process involved in drug absorption and distribution.FILTRATION1Filtration & Active transport: involved mainly in drug excretion L e c t u r eC y p e r s e c u r i t y 4M e 3 w a n 0 1Filtration DeF OF The passage of drugs through the water filled pores in the cell membranes by osmotic pressure gradient. Pressure gradient.Characteristics of drugs diffuse by filtration Water soluble Small size Unbound to plasma protein. Drug passage across cell membranes depends on :1 Size of drug particles Smaller drug particles can pass through the membrane easily.2 Lipid solubility The more lipid soluble the drug is, the easier to pass through the membrane.3 Degree of ionization unionized drugs can cross cell membrane more easily than ionized drugs. depends on pKa of the drug, nature of the drug (acidic or basic) and pH of the medium. p K a o f t h e d r u g & p H o f t h e m e d i u m .M C Q Unionized form is lipid soluble. Ionized form is water soluble. Lipid solubility of the drug depend on degree of ionization
P h a r m a c o l o g yG e n e r a l p h a r m a c o l o g yStudy today, save lives tomorrow. | Every page you read brings you closer to becoming a doctor. | Small daily progress leads to great medical achievements. | Knowledge is the first step toward healing. | Never stop learning because medicine never stops evolving. | Your future as a doctor is built by what you learn today. | Dream big, study hard, heal humanity. | Every page brings you one step closer to your white coat. | Discipline builds the doctor that motivation only dreams of. | Every hour of study is an investment in your future patients. | Stay focused. Stay determined. Stay committed to medicine. | Behind every great doctor is a history of hard work. | Learn something new every day; your future patients will thank you. | Great doctors are built through years of learning. | Believe in yourself, trust the process, and keep studying. | The more you learn, the better you serve. | Success in medicine begins with preparation. | Every medical book is a step toward saving lives. | Your only competition is yesterday's version of yourself. | Study with purpose. Practice with confidence. Heal with compassion. | Don't give up. Every chapter brings you closer to your dream. | Medical excellence is the result of consistent effort. | Every .lecture is a step toward becoming the doctor you aspire to be. | Focus on progress, not perfection. | Today's student, tomorrow's healerM o d u l e | F o u n d a t i o n 2 P h a r m a c o l o g yMS1M e d i c a l S t u d e n t sF i r s t - y e a rpKa of the drug (ionization constant )Acid Acid → unionized → lipid soluble → well absorbed & poorly excreted. Base Base → unionized → lipid soluble → well absorbed &poorly excreted. Acid Base → ionized → poorly absorbed & highly excreted.Acidic drugs 1 (e.g. Aspirin, pKa 3.5) → mostly unionized in stomach & upper part of small intestine, so well absorbed there.Basic drugs 2 (e.g. Atropine, pKa 10) → mostly absorbed in lower parts of the intestines. M C Q S A Q DeÜeÇie ÏiÜe f abÏ ÇÄÜi f dÇìgÏ:0 1 L e c t u r eC y p e r s e c u r i t y 5M e 3 w a n 0 1Degree of ionization is determined by pKa of the drug Nature of the drug (weak acids or weak bases) pH of the medium. It is the pH at which 50% of the drug is ionized and 50% is unionized” e.g: pKa of aspirin 3.5. I m p o r t a n c e o r c l i n i c a l s i g n i f i c a n c e
P h a r m a c o l o g yIV rout has 100% bioavailability. Oral rout bioavailability is variable.G e n e r a l p h a r m a c o l o g yStudy today, save lives tomorrow. | Every page you read brings you closer to becoming a doctor. | Small daily progress leads to great medical achievements. | Knowledge is the first step toward healing. | Never stop learning because medicine never stops evolving. | Your future as a doctor is built by what you learn today. | Dream big, study hard, heal humanity. | Every page brings you one step closer to your white coat. | Discipline builds the doctor that motivation only dreams of. | Every hour of study is an investment in your future patients. | Stay focused. Stay determined. Stay committed to medicine. | Behind every great doctor is a history of hard work. | Learn something new every day; your future patients will thank you. | Great doctors are built through years of learning. | Believe in yourself, trust the process, and keep studying. | The more you learn, the better you serve. | Success in medicine begins with preparation. | Every medical book is a step toward saving lives. | Your only competition is yesterday's version of yourself. | Study with purpose. Practice with confidence. Heal with compassion. | Don't give up. Every chapter brings you closer to your dream. | Medical excellence is the result of consistent effort. | Every .lecture is a step toward becoming the doctor you aspire to be. | Focus on progress, not perfection. | Today's student, tomorrow's healerM o d u l e | F o u n d a t i o n 2 P h a r m a c o l o g yMS1M e d i c a l S t u d e n t sF i r s t - y e a rAcidic drugs → ionized in alkaline urine ↑ excretion (e.g. aspirin toxicity → alkalinize urine).M C Q S A Q BIOAVAILABILITY2DefiiÜi I TÇaÄÄig:0 2 L e c t u r eC y p e r s e c u r i t y 6M e 3 w a n 0 1 Unionized acidic drugs (e.g. Aspirin) cross gastric mucosal cells. Inside cells (pH 7.0) they become ionized and get trapped. This leads to slow diffusion out and may cause gastric cell damage. DÇìg T iciÜ TÇeaÜeÜ:0 3Basic drugs → ionized in acidic urine ↑ excretion (e.g. amphetamine toxicity → acidify urine).Q u e s t i o n . . . ? What’s bioavailability? It is the percentage (fraction (F)) of the administered dose of a drug that reaches the systemic circulation in the unchanged form after any route of administration.exampleif 100 mg of a drug are administered orally and 70 mg of this drug are absorbed unchanged, the bioavailability of this drug is 70%.
P h a r m a c o l o g y2Shape and size of particles:1Dosage form: Solution > suspension > tablets.G e n e r a l p h a r m a c o l o g yStudy today, save lives tomorrow. | Every page you read brings you closer to becoming a doctor. | Small daily progress leads to great medical achievements. | Knowledge is the first step toward healing. | Never stop learning because medicine never stops evolving. | Your future as a doctor is built by what you learn today. | Dream big, study hard, heal humanity. | Every page brings you one step closer to your white coat. | Discipline builds the doctor that motivation only dreams of. | Every hour of study is an investment in your future patients. | Stay focused. Stay determined. Stay committed to medicine. | Behind every great doctor is a history of hard work. | Learn something new every day; your future patients will thank you. | Great doctors are built through years of learning. | Believe in yourself, trust the process, and keep studying. | The more you learn, the better you serve. | Success in medicine begins with preparation. | Every medical book is a step toward saving lives. | Your only competition is yesterday's version of yourself. | Study with purpose. Practice with confidence. Heal with compassion. | Don't give up. Every chapter brings you closer to your dream. | Medical excellence is the result of consistent effort. | Every .lecture is a step toward becoming the doctor you aspire to be. | Focus on progress, not perfection. | Today's student, tomorrow's healerM o d u l e | F o u n d a t i o n 2 P h a r m a c o l o g yMS1M e d i c a l S t u d e n t sF i r s t - y e a r3Rates of disintegration and dissolution of tablets: Rapid rate more absorptionPhysico-chemical properties:A1Lipid solubility: lipid soluble > water soluble2Degree of ionization : unionized> ionized3Stability of gastric acid and enzymes4Valency : (Fe²⁺) > (Fe³⁺). Pharmaceutical preparation5Nature : Inorganic > organic Pa t i e n t fa c t o r s2AI.V& inhalation >I.M > S.C> Oral> skin.B L e c t u r eC y p e r s e c u r i t y 7M e 3 w a n 0 1 Factors affecting oral Bioavailability D r u g Fa c t o r s1B Route of administration: Systemic circulation:Shock and heart failure ↓ absorption.
P h a r m a c o l o g yG e n e r a l p h a r m a c o l o g yStudy today, save lives tomorrow. | Every page you read brings you closer to becoming a doctor. | Small daily progress leads to great medical achievements. | Knowledge is the first step toward healing. | Never stop learning because medicine never stops evolving. | Your future as a doctor is built by what you learn today. | Dream big, study hard, heal humanity. | Every page brings you one step closer to your white coat. | Discipline builds the doctor that motivation only dreams of. | Every hour of study is an investment in your future patients. | Stay focused. Stay determined. Stay committed to medicine. | Behind every great doctor is a history of hard work. | Learn something new every day; your future patients will thank you. | Great doctors are built through years of learning. | Believe in yourself, trust the process, and keep studying. | The more you learn, the better you serve. | Success in medicine begins with preparation. | Every medical book is a step toward saving lives. | Your only competition is yesterday's version of yourself. | Study with purpose. Practice with confidence. Heal with compassion. | Don't give up. Every chapter brings you closer to your dream. | Medical excellence is the result of consistent effort. | Every .lecture is a step toward becoming the doctor you aspire to be. | Focus on progress, not perfection. | Today's student, tomorrow's healerM o d u l e | F o u n d a t i o n 2 P h a r m a c o l o g yMS1M e d i c a l S t u d e n t sF i r s t - y e a rAbsorbing surface:C1Surface area: Alveoli > intestine.2Vascularity : Alveoli > skeletal muscle > subcutaneous.3State of health.D Specific factors:↓ Intrinsic factor → ↓ B12E Presence of food or other drugsMilk (calcium) → ↓ absorption of tetracycline1 Gut first pass effect:A1 Gastric acidity : destroys benzyl penicillin.2 Digestive enzymes : destroy insulin. Hepatic first pass effect:B1 Drugs extensively metabolized : e . g . Nitroglycerine & Lidocaine2 Drugs metabolized to a large extent: e.g. propranololAbsorptionPortal veinGut wallTo faecesTo faecesMetabolismMetabolismBioavailabilityLiverPicture credit: Nature Reviews L e c t u r eC y p e r s e c u r i t y 8M e 3 w a n 0 13 First pass metabolism (presystemic elimination) Means metabolism of drug in gut wall or liver before reaching systemic circulation.F i r s t p a s s e f f e c t :
P h a r m a c o l o g yG e n e r a l p h a r m a c o l o g yStudy today, save lives tomorrow. | Every page you read brings you closer to becoming a doctor. | Small daily progress leads to great medical achievements. | Knowledge is the first step toward healing. | Never stop learning because medicine never stops evolving. | Your future as a doctor is built by what you learn today. | Dream big, study hard, heal humanity. | Every page brings you one step closer to your white coat. | Discipline builds the doctor that motivation only dreams of. | Every hour of study is an investment in your future patients. | Stay focused. Stay determined. Stay committed to medicine. | Behind every great doctor is a history of hard work. | Learn something new every day; your future patients will thank you. | Great doctors are built through years of learning. | Believe in yourself, trust the process, and keep studying. | The more you learn, the better you serve. | Success in medicine begins with preparation. | Every medical book is a step toward saving lives. | Your only competition is yesterday's version of yourself. | Study with purpose. Practice with confidence. Heal with compassion. | Don't give up. Every chapter brings you closer to your dream. | Medical excellence is the result of consistent effort. | Every .lecture is a step toward becoming the doctor you aspire to be. | Focus on progress, not perfection. | Today's student, tomorrow's healerM o d u l e | F o u n d a t i o n 2 P h a r m a c o l o g yMS1M e d i c a l S t u d e n t sF i r s t - y e a r12Increase the dose of the drug propranolol.D i s t r i b u t i o n0 2DefiiÜi Q u e s t i o n . . . ?What is the definition of Distribution?V o l u m e o f D i s t r i b u t i o n ( V d )DefiiÜi It is the volume of body fluids required to contain the total amount of drug in the body at the same concentration as in plasma.Vd =DoseC OM+M-MCMR789÷456×230=1-•CacìaÜi 9Vd = L e c t u r eC y p e r s e c u r i t yM e 3 w a n 0 1 Change route of administration lidocaine, penicillin& insulin (injections), Nitroglycerin (sublingual).Q u e s t i o n . . . ? How to avoid?A Is the process by which a drug leaves the bloodstream and enters the extracellular fluids and tissues of the body Or Disposition of a drug throughout the body from the general circulation Total dose (IV) Initial plasma concentration (C₀)
P h a r m a c o l o g yG e n e r a l p h a r m a c o l o g yStudy today, save lives tomorrow. | Every page you read brings you closer to becoming a doctor. | Small daily progress leads to great medical achievements. | Knowledge is the first step toward healing. | Never stop learning because medicine never stops evolving. | Your future as a doctor is built by what you learn today. | Dream big, study hard, heal humanity. | Every page brings you one step closer to your white coat. | Discipline builds the doctor that motivation only dreams of. | Every hour of study is an investment in your future patients. | Stay focused. Stay determined. Stay committed to medicine. | Behind every great doctor is a history of hard work. | Learn something new every day; your future patients will thank you. | Great doctors are built through years of learning. | Believe in yourself, trust the process, and keep studying. | The more you learn, the better you serve. | Success in medicine begins with preparation. | Every medical book is a step toward saving lives. | Your only competition is yesterday's version of yourself. | Study with purpose. Practice with confidence. Heal with compassion. | Don't give up. Every chapter brings you closer to your dream. | Medical excellence is the result of consistent effort. | Every .lecture is a step toward becoming the doctor you aspire to be. | Focus on progress, not perfection. | Today's student, tomorrow's healerM o d u l e | F o u n d a t i o n 2 P h a r m a c o l o g yMS1M e d i c a l S t u d e n t sF i r s t - y e a r25L<Vd<15LIn interstitial fluid. DÇìg DiÏÜÇibìÜi :0 1 V d < 5 L i n b l o o d . 5 L < V d < 1 5 L I n t e r s t i t i a l f l u i dIt is a theoretical or apparent volume of body fluids. It relates the concentration of a drug in the plasma to the total amount of the drug in the body. Vd is abstract concept, which determines where a drug is distributed. Vd<5 LDrug mainly in blood. L e c t u r eC y p e r s e c u r i t y 10M e 3 w a n 0 1IÜeÇÄÇeÜaÜi :13 Large Vd (>15 L)intracellular distribution (tissues reservoir → long action) C l i n i c a l s i g n i f i c a n c e o f V d :1Small Vd → Minimal distribution2Large Vd (>15 L) → intracellular distribution T iciÜ ÜÇeaÜeÜ:0 21Dialysis useful only for drugs with small Vd (e.g. Aspirin —mostly in circulation).
P h a r m a c o l o g yG e n e r a l p h a r m a c o l o g yStudy today, save lives tomorrow. | Every page you read brings you closer to becoming a doctor. | Small daily progress leads to great medical achievements. | Knowledge is the first step toward healing. | Never stop learning because medicine never stops evolving. | Your future as a doctor is built by what you learn today. | Dream big, study hard, heal humanity. | Every page brings you one step closer to your white coat. | Discipline builds the doctor that motivation only dreams of. | Every hour of study is an investment in your future patients. | Stay focused. Stay determined. Stay committed to medicine. | Behind every great doctor is a history of hard work. | Learn something new every day; your future patients will thank you. | Great doctors are built through years of learning. | Believe in yourself, trust the process, and keep studying. | The more you learn, the better you serve. | Success in medicine begins with preparation. | Every medical book is a step toward saving lives. | Your only competition is yesterday's version of yourself. | Study with purpose. Practice with confidence. Heal with compassion. | Don't give up. Every chapter brings you closer to your dream. | Medical excellence is the result of consistent effort. | Every .lecture is a step toward becoming the doctor you aspire to be. | Focus on progress, not perfection. | Today's student, tomorrow's healerM o d u l e | F o u n d a t i o n 2 P h a r m a c o l o g yMS1M e d i c a l S t u d e n t sF i r s t - y e a rCacìaÜi Ï:0 31Loading dose = Vd × Desired concentration.1↓ Albumin (malnutrition, pregnancy) → ↑ free drug → toxicity (e.g. Phenytoin).2t 1/2 = 0.693 × Vd / Clearance. Factors affecting the distribution of drugs11Drugs exist in 2 forms:2Drug displacement by another with higher affinity (Drug interaction) e.g. (NSAIDS displace warfarin and sulfonylurea)3Renal failure → changes drug protein affinity L e c t u r eC y p e r s e c u r i t y 11M e 3 w a n 0 1 P h y s i co c h e m i ca l p ro p e r t i es1 Size the smaller the larger vd. Solubility lipid soluble drugs have large vd. B i n d i n g t o p l a s m a p rot e i n s :21 Free form2 Bound formactive distributed. metabolized excreted. inactive acts as reservoir prolong duration of action of drug.N O T D i s t r i b u t e d M e t a b o l i z e d E x c r e t e d A c t i v e Factors altering binding
P h a r m a c o l o g yG e n e r a l p h a r m a c o l o g yStudy today, save lives tomorrow. | Every page you read brings you closer to becoming a doctor. | Small daily progress leads to great medical achievements. | Knowledge is the first step toward healing. | Never stop learning because medicine never stops evolving. | Your future as a doctor is built by what you learn today. | Dream big, study hard, heal humanity. | Every page brings you one step closer to your white coat. | Discipline builds the doctor that motivation only dreams of. | Every hour of study is an investment in your future patients. | Stay focused. Stay determined. Stay committed to medicine. | Behind every great doctor is a history of hard work. | Learn something new every day; your future patients will thank you. | Great doctors are built through years of learning. | Believe in yourself, trust the process, and keep studying. | The more you learn, the better you serve. | Success in medicine begins with preparation. | Every medical book is a step toward saving lives. | Your only competition is yesterday's version of yourself. | Study with purpose. Practice with confidence. Heal with compassion. | Don't give up. Every chapter brings you closer to your dream. | Medical excellence is the result of consistent effort. | Every .lecture is a step toward becoming the doctor you aspire to be. | Focus on progress, not perfection. | Today's student, tomorrow's healerM o d u l e | F o u n d a t i o n 2 P h a r m a c o l o g yMS1M e d i c a l S t u d e n t sF i r s t - y e a r1Thiopental sodium brain &fat Tetracycline bone & teeth.311 Re d i s t r i b u t i o n of d r u g s5 occur with occur with highly lipid soluble drugs as thiopental. Thiopental (highly lipid-soluble drug used in general anesthesia): Accumulates first in brain (high lipid solubility + high blood flow). Then redistributes to fat (poorly perfused Af f i n i t y t o d i f fe re n t t i s s u es L e c t u r eC y p e r s e c u r i t y 12M e 3 w a n 0 1Well-perfused organs (high blood flow) as Brain, Heart, Kidneys and Splanchnic organs Achieve high drug levels faster than poorly perfused tissues (e.g. fat, bone). B l o o d f l ow4 Give reason: Although Thiopental has a long half-life, its duration of action is short (~10 min).C linic a l I m p o r t a n c e : Duration of action of some drugs as Thiopental Not determined by metabolism or excretion Determined by rate of redistribution
P h a r m a c o l o g yG e n e r a l p h a r m a c o l o g yStudy today, save lives tomorrow. | Every page you read brings you closer to becoming a doctor. | Small daily progress leads to great medical achievements. | Knowledge is the first step toward healing. | Never stop learning because medicine never stops evolving. | Your future as a doctor is built by what you learn today. | Dream big, study hard, heal humanity. | Every page brings you one step closer to your white coat. | Discipline builds the doctor that motivation only dreams of. | Every hour of study is an investment in your future patients. | Stay focused. Stay determined. Stay committed to medicine. | Behind every great doctor is a history of hard work. | Learn something new every day; your future patients will thank you. | Great doctors are built through years of learning. | Believe in yourself, trust the process, and keep studying. | The more you learn, the better you serve. | Success in medicine begins with preparation. | Every medical book is a step toward saving lives. | Your only competition is yesterday's version of yourself. | Study with purpose. Practice with confidence. Heal with compassion. | Don't give up. Every chapter brings you closer to your dream. | Medical excellence is the result of consistent effort. | Every .lecture is a step toward becoming the doctor you aspire to be. | Focus on progress, not perfection. | Today's student, tomorrow's healerM o d u l e | F o u n d a t i o n 2 P h a r m a c o l o g yMS1M e d i c a l S t u d e n t sF i r s t - y e a rBlood-Brain Barrier (BBB):1 (BBB, Placental barrier, Breast milk): lipid solubility state of the barrier (normal vs inflamed). Placental barrier:2Non-ionized lipid-soluble drugs can cross the placental barrier and affect the fetus. Examples. most antibiotics Possible effects of drugs crossing the placenta: During pregnancy: Teratogenicity (e.g. tetracycline). During labor: Neonatal asphyxia (e.g. morphine).3 Passage of drugs through breast milkpH Difference: Most drugs administered to lactating women are detectable in breast milk. Non-ionized, lipid-soluble drugs easily pass the BBB and affect the CNS. Some hydrophilic antibiotics (e.g. Penicillin) can pass only during meningitis Drug passage through BBB depends mainly on L e c t u r eC y p e r s e c u r i t y 13M e 3 w a n 0 1 Pa s s a g e of d r u g s a c ros s b a r r i e r s5 Milk pH ≈ 7.0 (more acidic) Plasma pH ≈ 7.4 Basic drugs become ionized & accumulate in milk → “Ion Trapping” Basic and lipid-soluble drugs are most likely to appear in breast milk
P h a r m a c o l o g yG e n e r a l p h a r m a c o l o g yStudy today, save lives tomorrow. | Every page you read brings you closer to becoming a doctor. | Small daily progress leads to great medical achievements. | Knowledge is the first step toward healing. | Never stop learning because medicine never stops evolving. | Your future as a doctor is built by what you learn today. | Dream big, study hard, heal humanity. | Every page brings you one step closer to your white coat. | Discipline builds the doctor that motivation only dreams of. | Every hour of study is an investment in your future patients. | Stay focused. Stay determined. Stay committed to medicine. | Behind every great doctor is a history of hard work. | Learn something new every day; your future patients will thank you. | Great doctors are built through years of learning. | Believe in yourself, trust the process, and keep studying. | The more you learn, the better you serve. | Success in medicine begins with preparation. | Every medical book is a step toward saving lives. | Your only competition is yesterday's version of yourself. | Study with purpose. Practice with confidence. Heal with compassion. | Don't give up. Every chapter brings you closer to your dream. | Medical excellence is the result of consistent effort. | Every .lecture is a step toward becoming the doctor you aspire to be. | Focus on progress, not perfection. | Today's student, tomorrow's healerM o d u l e | F o u n d a t i o n 2 P h a r m a c o l o g yMS1M e d i c a l S t u d e n t sF i r s t - y e a rSAQShort answer QuestionsL e c t u r eC y p e r s e c u r i t y 14M e 3 w a n 0 1 0 1 Define pKa and list two of its clinical significance? 0 2 Define 1st pass metabolism and how to avoid it? 0 3 Discuss passage of drugs into Breast milk? 0 4 Give reason (accumulation of lipid-soluble and basic drugs more likely to accumulate in milk) 0 5 Discuss clinical significance of Vd. 0 6 Define Vd and how to calculate it? 0 7 Give reason [ Although Thiopental has a long halflife, its duration of action is short (~10 min)]. 0 8 Define bioavailability and list three factors that affect it?
P h a r m a c o l o g yG e n e r a l p h a r m a c o l o g yStudy today, save lives tomorrow. | Every page you read brings you closer to becoming a doctor. | Small daily progress leads to great medical achievements. | Knowledge is the first step toward healing. | Never stop learning because medicine never stops evolving. | Your future as a doctor is built by what you learn today. | Dream big, study hard, heal humanity. | Every page brings you one step closer to your white coat. | Discipline builds the doctor that motivation only dreams of. | Every hour of study is an investment in your future patients. | Stay focused. Stay determined. Stay committed to medicine. | Behind every great doctor is a history of hard work. | Learn something new every day; your future patients will thank you. | Great doctors are built through years of learning. | Believe in yourself, trust the process, and keep studying. | The more you learn, the better you serve. | Success in medicine begins with preparation. | Every medical book is a step toward saving lives. | Your only competition is yesterday's version of yourself. | Study with purpose. Practice with confidence. Heal with compassion. | Don't give up. Every chapter brings you closer to your dream. | Medical excellence is the result of consistent effort. | Every .lecture is a step toward becoming the doctor you aspire to be. | Focus on progress, not perfection. | Today's student, tomorrow's healerM o d u l e | F o u n d a t i o n 2 P h a r m a c o l o g yMS1M e d i c a l S t u d e n t sF i r s t - y e a rGive Reason: Although Thiopental has a long half-life, its duration of action is short (~10 min)? L e c t u r eC y p e r s e c u r i t y 15M e 3 w a n 0 1Because it is a highly lipid-soluble → rapidly enters the brain (high blood flow) → causes anesthesia. Then it redistributes from the brain to less-perfused tissues like fat and muscle. leading to a rapid fall in brain concentration and recovery of consciousness.S u m m a r y . . . . Short action due to redistribution, not metabolism or excretion.McQ Multiple-Choice Questions 0 1 Distribution is the: PÇ ceÏÏ ÜhaÜ defieÏ Ühe dÇìg eÜÇace iÜ Ühe ÏÏÜeic ciÇcìaÜi fÇ Ühe ÏiÜe f adiiÏÜÇaÜi Ç aÄÄicaÜi A AbÏÜÇacÜ c ceÄÜ, hich deÜeÇieÏ heÇe iÏ a dÇìg diÏÜÇibìÜedB Cheica ÄÇ ceÏÏig f dÇìgÏ bef Çe Ühe i eae a ÇgaiÏ.C DiÏÄ ÏiÜi f a dÇìg ÜhÇ ìgh ìÜ Ühe b d fÇ Ühe geeÇa ciÇcìaÜi D EiiaÜi f dÇìgÏ fÇ Ühe b d.E 0 2 Drugs that are more likely to accumulate in breast milk are:A BaÏic ad iÄid Ï ìbe.B Acidic ad iÄid iÏ ìbe.C NeìÜÇa ad ÄaÏa ÄÇ Üei b ìd.D Acidic ad iÄid Ï ìbe.E Acidic ad aÜeÇ-Ï ìbe.
P h a r m a c o l o g yG e n e r a l p h a r m a c o l o g yStudy today, save lives tomorrow. | Every page you read brings you closer to becoming a doctor. | Small daily progress leads to great medical achievements. | Knowledge is the first step toward healing. | Never stop learning because medicine never stops evolving. | Your future as a doctor is built by what you learn today. | Dream big, study hard, heal humanity. | Every page brings you one step closer to your white coat. | Discipline builds the doctor that motivation only dreams of. | Every hour of study is an investment in your future patients. | Stay focused. Stay determined. Stay committed to medicine. | Behind every great doctor is a history of hard work. | Learn something new every day; your future patients will thank you. | Great doctors are built through years of learning. | Believe in yourself, trust the process, and keep studying. | The more you learn, the better you serve. | Success in medicine begins with preparation. | Every medical book is a step toward saving lives. | Your only competition is yesterday's version of yourself. | Study with purpose. Practice with confidence. Heal with compassion. | Don't give up. Every chapter brings you closer to your dream. | Medical excellence is the result of consistent effort. | Every .lecture is a step toward becoming the doctor you aspire to be. | Focus on progress, not perfection. | Today's student, tomorrow's healerM o d u l e | F o u n d a t i o n 2 P h a r m a c o l o g yMS1M e d i c a l S t u d e n t sF i r s t - y e a rL e c t u r eC y p e r s e c u r i t y 16M e 3 w a n 0 1 0 3 If the total amount of a drug present in the body at a given moment is 2 g and its plasma concentration is 25 mg/L, its volume of distribution is:A 80 L .B 60LC 50LD 30LE 100L 0 4 What does “pharmacokinetics” includeA UaÜed effecÜÏ f dÇìgÏ.B Cheica ÏÜÇìcÜìÇe f a edicia ageÜ.C DiÏÜÇibìÜi f dÇìgÏ i Ühe ÇgaiÏ.D Ifìece f dÇìgÏ geeÏ.E PhaÇac gica effecÜÏ f dÇìgÏ. 0 5 The phenomenon where basic drugs accumulate in breast milk due to pH difference is calledA FaÜ ÇeÜeÜi .B I ÜÇaÄÄig.C PaÏa ÄÇ Üei bidig.D FiÜÇaÜi E SiÄe diffìÏi . 0 6 Find correct definition to presystemic metabolism (first pass metabolism). DÇìg iacÜiaÜi i Ühe ÏÏÜeic ciÇcìaÜi .A DÇìg iacÜiaÜi i ~ideÏ.B DÇìg iacÜiaÜi i Ühe ieÇ afÜeÇ ÏÏÜeic ciÇcìaÜi .C DÇìg iacÜiaÜi i Ühe gaÏÜÇ iÜeÏÜia ìe, gìÜ a, ad i Ühe ieÇ.D EcÇeÜi f Ühe dÇìg i bie.E