UNIT 1: INTRODUCTION APPLICATION OF PHARMACEUTICAL BIOCHEMISTRY • The study of chemical substances found in living organisms and the chemical interactions of • Drug delivery – 10 to 80 mg these substances with each other. daily, check lipid levels after 2-4 - Molecules in living cell. weeks and adjust dose. - Chemical reactions. • Pharmacokinetics - absorption - Catalyst in reaction. rate varies from 30-85% following per oral - Metabolic process. administration. BIOCHEMICAL SUBSTANCES • Clinical Pharmacology – first line of treatment • Biochemical substance is a chemical substance for atherosclerotic cardiovascular disease found within a living organism. (ASCVD) and hyperlipidemia. • Bioinorganic substances – do not contain • Enzymology – inhibitor of HMG CoA reductase, carbon. the rate limiting step in cholesterol synthesis. - Water: 70% • Pharmacodynamics – depletion of intercellular - Inorganic salts: 5% cholesterol but elevated liver enzymes may • Bioorganic substances – contains carbon. occur. - Protein: 15% - Lipids: 8% ESSENCE OF BIOCHEMISTRY IN LIFE • Genetics - Carbohydrates: 2% - Biochemistry of nucleic acid. - Nucleic acid: 2% - Approaches to understand disease. BRANCHES OF BIOCHEMISTRY - Familial hypercholesterolemia: • Medical Biochemistry understanding cell receptors cellular uptake - Related to human health and disease. mechanism of cholesterol. - Functioning of traditional and pathologic - Pharmacogenetics: genes involved in disease. changing drug metabolic rate. - Operation and management of o Genes can affect the drugs so other laboratories. person are not suitable with some drug. - Directs clinical laboratories, consults, • Physiology diagnoses, and treats patient. - Chemical changes relate to physiological • Clinical Chemistry alteration in the body. - A field that focuses on the methodology - Oncogenes: how cell/genes work in the body. and interpretation of chemical tests • Immunology performed to support diagnosis and - Provides qualitative and quantitative analysis treatment. of biological fluids useful for evaluation of • Pharmaceutical Biochemistry immune factors. - Involves how drugs affect the biochemistry - Use of antibodies in convalescent plasma and metabolism of human health and therapy against COVID-19. sickness. - Study of immune system by fluids. - Production of medicines. • Pharmacology - Understanding of chemical process. - Most drugs are metabolized by enzyme- - Clinical uses and adverse effects. catalyzed reactions. - Molecular targets and characterization. - Suggest rational treatments. - Drug delivery: drug dosage - Assist in monitoring to their illness. • Toxicology - Enzymology: study of enzymes - Routine examination of blood chemistry. - Pharmacokinetics: how drug works - Metabolic fate of poisons. - Pharmacodynamics: affect of drug. - Stage and effects to organs. - Clinical pharmacology: research - Mechanism of toxicity.
Prepared by: M. SALAZAR & J. AGBUYA
Bachelor of Science in Pharmacy 1|Page School of Natural Sciences Saint Louis University S REVIEWER FOR BACHELOR OF SCIENCE IN PHARMACY PROFESSIONAL SUBJECTS AND BOARD EXAMS Nutritional Deficiencies, excesses • Pathology Imbalance - Reveal the fundamental causes Endocrine Hormonal deficiencies, mechanisms. imbalance excesses - Diagnoses of diseases thru procedures acting Immunologic Anaphylaxis, autoimmune as screening tests. Reaction disease - Affect the alteration. • Biochemistry and Medicine • Medicine o Nucleic Acid (smallest) – Genetic - Understanding and maintenance of health. diseases. - Understanding and effective treatment of o Proteins – sickle cell anemia. diseases. o Biochemistry – medicine - Treatment, medication, cure, prevention o Lipids – atherosclerosis - Protein structure and function o Inherited RBC disorder in which the o Carbohydrates (largest) – diabetes hemoglobin changes its shape that easily mellitus. lyses. USES OF BIOCHEMICAL STUDIES • To reveal the fundamental causes and SUMMARY OF CHAPTER 1: INTRODUCTION mechanisms of diseases • Biochemistry is the science concerned with - Nature and analysis of genetic diseases studying the various molecules with their such as cystic fibrosis and sickle cell anemia. chemical reactions. Because life depends on • To suggest rational treatments and diseases biochemical reactions, biochemistry has based on the fundamental causes and become the basic language of all biologic mechanism of diseases sciences. - A diet low in phenylalanine for treatment of phenylketonuria Atorvastatin for BIOCHEMISTRY AS BASIS OF HEALTH AND DISEASE hypercholesterolemia. • Depends on a harmonious balance or • To assist in diagnosis of specific diseases biochemical reactions occurring in the body. - Blood glucose level for diabetes mellitus. • Intra and extracellular reactions that occur are - Abnormally high serum creatinine for kidney proceeding organism’s maximal survival in problem. physiologic state. • To act as screening tests for the early diagnosis • Optimal intake of vitamins, certain amino acids, of certain diseases certain fatty acids, various minerals, and water. - Antenatal screening for prenatal diagnosis. • Systematic attempts to maintain health and - Neonatal screening for congenital forestall disease such as preventive medicine. hypothyroidism. • Biochemistry equals to health. • To assist in monitoring the progress of certain • Disease affects abnormalities in biomolecules, diseases biochemical reactions, or biochemical - Plasma enzyme ALT for infectious hepatitis. processes. Disease is not equal to health. - High glycated hemoglobin for longer term Physical agents Trauma, temperature, gauge of blood glucose control. atmospheric pressure, • To asses in assessing the response of disease to radiation, and electric shook. therapy Chemical agents Illicit drugs, therapeutic - High glycated hemoglobin for poor drugs, toxic compounds. response to hypoglycemic agent. Biologic agents Viruses, bacteria, fungi, - Renal and liver function tests for drug’s helminths, protozoa efficacy and detection of possible toxicity. Lack of oxygen Loss of blood supply, poisoning of the oxidative enzymes. Genetic Disorders Congenital, molecular, metabolic
Prepared by: M. SALAZAR & J. AGBUYA
Bachelor of Science in Pharmacy 2|Page School of Natural Sciences Saint Louis University S REVIEWER FOR BACHELOR OF SCIENCE IN PHARMACY PROFESSIONAL SUBJECTS AND BOARD EXAMS
Prepared by: M. SALAZAR & J. AGBUYA
Bachelor of Science in Pharmacy 3|Page School of Natural Sciences Saint Louis University S REVIEWER FOR BACHELOR OF SCIENCE IN PHARMACY PROFESSIONAL SUBJECTS AND BOARD EXAMS AMINO ACIDS - Zwitterion: amino (+) carboxylate (-) • Structure • Optical Activity - a-Carbon, amino - Enantiomers group, carboxyl - Polarimeter group, hydrogen, - Conformation side chain or R- - D-amino acid: (+) dextrorotatory (clockwise) group. - L-amino (-) levorotatory (counterclockwise) - Unionized form has no charge.
AMINO ACID ZWITTERION
• Formation of Peptides D-Alanine L-Alanine
- Condensation = Addition Reaction L-Isomer D-Isomer - Interaction between amino group of one a-amino with the carboxylic group of another a-amino. - Liberation of H2O - Dipeptide: two a-amino - Tripeptide: three a-amino - Proteins or polypeptides: longer peptide chains. - L (+) alanine is the L-enantiomer and it is • General Properties dextrorotatory. - Acid-base property also known as - L (-) Serine is the L-enantiomer and it is amphoteric levorotatory. - aa acid: H+ NH3 • Polarity - aa base: H+ COO- - Interaction with water. - Non-polar aa ADDITION OF ACID o Amino group, One carboxyl group, Non- polar side chain, Glycine, Alanine, Proline, Valine, Leucine, Isoleucine, ADDITION OF BASE Methionine, Tryptophan, phenyl alanine - Polar Neutral AA • Isoelectric point o One amino group, one carboxyl group, A side chain that is polar but neutral, Serine, Threonine, Cysteine, Asparagine, Glutamine, Tyrosine - Polar Acidic AA o One amino group o Two carboxyl group o Aspartic acid o Glutamic acid • Stereochemistry - Polar Basic AA - Different functional groups o Two amino groups - Enantiometers: non-superimposable o One carboxyl group - a-carbon: chiral carbon o Histidine, Arginine, Lysine - a-carbon: asymmetrical
Prepared by: M. SALAZAR & J. AGBUYA
Bachelor of Science in Pharmacy 4|Page School of Natural Sciences Saint Louis University S REVIEWER FOR BACHELOR OF SCIENCE IN PHARMACY PROFESSIONAL SUBJECTS AND BOARD EXAMS NAME SYMBOL ABV. STRUCTURE FUNCTIONAL GROUP ISOELECTRIC IN SIDE CHAIN POINT tyrosine Y Tyr phenolic-OH group 5.7
SIDE CHAIN COTAINS SULFUR
cysteine C Cys thiol 5.0
methionine M Met sulfide
SIDE CHAIN CONTAINS NONBASIC NITROGEN
asparagine N Asn amide 5.4
glutamine Q Gln amide 5.7
tryptophan W Trp indole 5.9
SIDE CHAIN IS ACIDIC
aspartic acid D Asp carboxylic acid 2.8
glutamic acid H Glu carboxylic acid 3.2
SIDE CHAIN IS BASIC
lysine K Lys amino group 9.7
arginine R Arg guanidino group 10.8
histidine H His imidazole ring 7.6
glycine G Gly none 6.0
alanine A Ala alkyl group 6.0
valine V Val alkyl group 6.0
leucine L Leu alkyl group 6.0
isoleucine I Ile alkyl group 6.0
phenylalanine F Phe aromatic group 5.5
proline P Pro rigid cyclic structure 6.3
serine S Ser hydroxyl group 5.7
threonine T Thr hydroxyl group 5.6
Prepared by: M. SALAZAR & J. AGBUYA
Bachelor of Science in Pharmacy 5|Page School of Natural Sciences Saint Louis University S