Inorganic Pharmaceutical Chemistry PDF Trial

MODULE 1│PHARM CHEM 1 INORGANIC PHARMACEUTICAL CHEMISTRY A. ABUNDANCE 2. Sodium – Na Def: Hyponatremia – “emia” – blood; low Na lev...

MODULE 1│PHARM CHEM 1 INORGANIC PHARMACEUTICAL CHEMISTRY A. ABUNDANCE 2. Sodium – Na Def: Hyponatremia – “emia” – blood; low Na levels 1. Element: Tox: Hypernatremia – (fluid retention) high Na levels 1st – O2 (non-metal) 2nd – Si (non-metal) 3. Potassium – K 3rd – Al (Most abundant metal) Def: Hypokalemia – lead to muscle paralysis (common causes: severe burns, diarrhea 2. Air Gas – N2 (Air = N2 + O2 [71:29]) Tox: Hyperkalemia – lead to Cardiac arrest (muscle contraction) 3. Noble gas – Ar (least abundant – Kr, Xe) KCl – use in mercy killing Ax: Sodium polystyrene sulfonate (Kayexalate®) – Cation 4. Intra- & Extracellular ions exchange resin Most abundant/ major/ principal/ 1° PISO (K+ IN, Na+ OUT 4. Copper – Cu PICO (HPO4-2 IN, Cl- OUT Tox: Wilson’s disease – bronze-like skin MICO (Mg2+ IN, Ca2+ OUT Ax: Penicillamine (Cuprimine®) 2nd most abundant/ minor/ 2° BIO (HCO3- OUT) 5. Silver – Ag HCO3- : H2CO3 – most important physiological buffer system Tox: Argyria (darkened skinned due to chronic use) Respiratory: CO2 (acidic) ↑ Acidosis Ax: NaCl (NSS) – isotonic (not painful when administered) ↓ Alkalosis Ag + NaCl → AgCl↓ Metabolic: HCO3- (basic) ↓ Acidosis (DOC: NaHCO3) ↑ Alkalosis 6. Gold – Au Dermatitis, Glossitis – inflammation of the tongue (PO) B. VITAMINS FOR MAXIMUM MINERAL ABSORPTION Ax: BAL “FeCaDSeE” 7. Calcium – Ca Fe – Vit. C; CuSO4 – blue vitriol (enhance Fe utilization) Def: Hypocalcemia Ca – Vit. D Defective bone mineralization – Rickets/ bowed legs in Se – Vit. E children; Osteomalacia in adults Defective bone resorption – Osteoporosis – brittle bone N2 Black cylinder Others: Muscle spasm → tetany, seizure NO2, N2O Blue cylinder Tox: Hypercalcemia – constipation: ↑ Ca levels Mg(OH)2 Blue bottle Ax: EDTA – converted into Ca EDTA (chelating agent) O2 Green cylinder Ar Dark green 8. Barium – Ba CO2 Grey Tox: Baritosis – Benign Pneumoconiosis (non-fibrotic) He Brown Ax: MgSO4 – converted into BaSO4 ↓ (non-absorbable) H2 Red Acetylene Maroon 9. Zinc – Zn Cl2 Yellow Def: Parakeratosis (scaly, thickened, & inflamed skin), Li Coated w/ petroleum or under oil (ra) impaired immunity White/Yellow P Under water Metal fume fever – due to inhalation of ZnO Ax: NaHCO3 D. GLASS 10. Cadmium – Cd Tox: Itai-itai disease or Ouch-ouch disease Silica + Na2CO3 Ax: Ca EDTA – Immediately given after exposure Mgt: Palliative therapy Glass Types I Highly Resistant Borosilicate (Pyrex, Borosil) Boron – decrease coefficient of expansion 11. Mercury – Hg (BEQ) II Treated Soda Lime Glass Neurotoxic: Minamata disease, pink disease (Acrodynia in III Soda Lime Glass; Dry Powder Packaging children) Mad hatter’s disease/ Erethism IV/NP General Soda Lime Glass Ax: *NP – not for parenteral Na formaldehyde sulfoxylate – best antidote; RA: Hg2+ → Hg22+ (less soluble) Leach tests (See QA/QC – RMCQ) DMSA (Succimer) – water soluble analog of BAL for all Water attack test – for type II types of Hg poisoning Powdered glass test – for type I & III Penicillamine (Cuprimine®) – Elemental Hg BAL – Inorg salts only Glass modification Ca EDTA K Brown/ amber, light resistant Se Red 12. Boric acid MnO2 Masks blue-green color Fe usu. present in glass Tox: Boiled lobster appearance – reddish-orange skin (PO/ B (as borate) Decrease coefficient of expansion dermal absorption) Pb Increase refractive index Rare earths Selectively absorb light of certain wavelengths 13. Aluminum – Al HF Glass etching Tox: Shaver’s disease/ Bauxite pneumoconiosis (inhalation), Alzheimer’s disease in elderly (Neurotoxic), Constipation E. INORGANIC: DEFICIENCIES & TOXICITIES (See Toxicology) (Ala-Tae) 1. Lithium – Li “MNOP” 14. Silicon – Si (Silicon dioxide – SiO2) Hypokalemia – movement disorder (tremor) Tox: Silicosis – TB-like Hyponatremia – Nephrogenic Diabetes insipidus – hence do (Pneumonoultramicroscopicsilicovolcanokoniosis) Resulting to not restrict Na intake; (polyuria) Hemoptysis – blood in sputum & lung irritation due to chronic Hypothyroidism inhalation Pregnancy problems (teratogenic) – Ebstein’s anomaly Ax: Alumina – adsorbents; forms coat w/ Silica part. Module 1 – Inorganic Pharmaceutical Chemistry Page 1 of 12 RJAV 2022 15. Lead – Pb F. INORGANIC: ANTIDOTES (See Toxicology) Tox: Plumbism/ Saturnism – wrist drop/ foot drop Ax: Ca EDTA/ Ca versenate (BEQ) 1. Activated charcoal + Tannic acid + MgO (2:1:1 Universal antidote (for weak acids & weak bases – drugs) 16. Zirconium – Zr CI: Household and Industrial poisons e.g., CN & Kerosene Tox: Granuloma in skin & lungs – Banned! poisoning 17. Phosphorus – P (white/ yellow) – General protoplasmic poison Activated charcoal Acute: Garlic breath odor, luminous vomitus, severe GI Destructive distillation residue of various org materials irritation (bloody diarrhea, liver damage) treated to increase adsorptive power Chronic: Bony necrosis, esp. in mandible (Phossy jaw) Official USP: Fine form Ax: Cupric sulfate, Ceric sulfate Adsorbent Antidiarrheal 18. Arsenic – As (lewisite metal) Acute: Aldrich-mee’s lines (white lines in fingernails), Garlic 2. Disodium EDTA/ Edetate disodium (C10H14N2Na2O8 2H2O) breath odor, luminous vomitus, severe GI irritation (bloody Ag proteinate stabilizer diarrhea) Emergency tx of hypercalcemia (IV) Chronic: Arsenicosis, Cancer S/E: Hypocalcemia rapidly develops Ax: British anti-lewisite (BAL/Dimercaprol) 3. Calcium disodium edetate/ Edetate calcium disodium 19. Bismuth – Bi (C10H12N2Na2CaO8) Blue-black gums Ax: for heavy metal poisoning (especially Lead – Pb) Black stools (Bi2S3) Adv: Does not precipitate Hypocalcemia BAL 4. Amyl nitrite + Na nitrite + Na thiosulfate 20. Vanadium – V CN antidote kit component Tox: Green tongue Supplemental: NaHCO3 – Metabolic acidosis 21. Sulfur – S (Sulfites, Sulfur dioxide – SO2) Hyperbaric/ 100% O2 (2-3 atm) – Tx. Hypoxia/ Hypersensitivity reactions – Angioedema, Bronchospasms, Asphyxia. Anaphylaxis - Industrial Prep: Fractional distillation of liquid air 22. Selenium – Se Other agents used in CN poisoning: Def: Keshan disease Methylene blue Tox: Contact dermatitis Hydroxocobalamin 23. Chromium – Cr G. RADIOPHARMACEUTICALS Hyperglycemia (DM-like) 1. Liver (BEQ) 24. Fluorine – F Tc99m IDA (Imino diacetic acid) – Hepatobiliary studies Tox: Dental (enamel mottling) & Skeletal fluorosis Tc99m phytate – Liver imaging for potency studies HF, F- salts: Slow-healing burns Au198 – Liver scanning Ax: Ca gluconate → CaF2 ppt (non-absorbable) I131 Rose Bengal – tracer of liver function Na iodohippurate – Diagnosis of Liver function 25. Bromine – Br (depressant property) Tox: Bromism (Psychosis, skin eruption, headache, 2. Kidney weakness) Tc99m heptagluconate – Kidney imaging for Renal function Ax: Na/ NH4Cl → NaBr ppt determination Hg197 chlormerodrin – Kidney & Brain scintillation scanning 26. Iodine – I Def: Simple/ colloid goiter: Caution to pregnant → Cretinism 3. Heart – lead to congenital hypothyroidism Tc99m sestamibi/ methoxy isobutyl isonitrile – Myocardial Tox: Iodism (acute), hypothyroidism (chronic) – negative perfusion agent feedback effect I131 NaI – Cardiac output determination – blood plasma vol. Ax: Starch solution (starch-iodo complex: dark blue), NaCl, Na thiosulfate (iodometry – indirect method for Iodine 4. Thyroid determination) Tc99m pertechnetate – Thyroid scanning I125 NaI – Diagnosis of Thyroid function 27. Manganese – Mn Parkinson-like (tremors) 5. Others: Tc99m etidronate/ phosphonates – Bone imaging 28. Helium – He Tc99m macro aggregated albumin – Lung scanning Donald duck sound Cr51 – Spleen imaging, RBC mass P32 Na phosphate – Treatment of Polycythemia vera 29. Iron – Fe Co57 cyanocobalamin – Diagnosis of Pernicious anemia Tox: GI irritation (black stools) Fe2S3, Hemochromatosis, (high RBC) Cardiac collapse Se75 selenomethionine – Diagnosis of Pancreatic tumors Ax: Deferoxamine H. IMPORTANT ALLOYS: 30. Cobalt – Co Def: Megaloblastic anemia/ Macrocytic anemia (B9 & B12) Plumber’s Solider 67% Pb, 33% Sn Ax: Hydroxocobalamin, Cyanocobalamin (Vit B12) Solder 50 % Pb, 50% Sn Pewter 20% Pb, 80% Sn 31. Nickel – Ni Babbitt 20% Sb, 80% Sn Tox: Nickel itch – contact dermatitis Type metal 50% Pb, 25% Sn, 25% Sb Rose metal 25% Pb, 25% Sn, 50% Bi Bronze Copper + Sn Gun metal Copper + Sn (90 : 10) Anti-friction Metal Copper + Sn + Sb (12.5 : 75 : 12.5) Brass Copper + Zn Module 1 – Inorganic Pharmaceutical Chemistry Page 2 of 12 RJAV 2022  Monel Copper + Ni Ammonium (NH4+) German Silver Copper + Ni + Zn Weak base Sterling Silver Copper + Ag (7.5 : 92.5) Hypothetical/ pseudo alkali metal Raney Nickel Aluminum + Ni Pharmacological use: Diuretic, expectorant, buffer Steel Iron + 3% C component Misch Metal Iron + 70% Ce Woods Metal* Cd, Sn, Pb, Bi (12.5 : 12.5 : 25 : 50) Compounds Ammonia, NH3 - Respiratory stimulant (pungent I. COLORS OF TRANSITION METAL IONS IN Aq. SOLUTION odor) - Basic (blue litmus) Based on oxidation state Household ammonia - 10% or 16° (degree Baume) NH3 Dilute ammonia solution; - 9.5-10.5% NH3 Cu +2 = Blue ammonia water - Neutralize insect/ jellyfish stings Cr +2 = Blue Strong ammonia solution/ water - 27-31% NH3 +3 = Green (Spirit of Hartshorn) +6 = Chromate: Cr2O4-2 (Yellow), Aromatic ammonia spirit (Spirit of - Strong ammonia soln + ammonium Dichromate: Cr2O7-2 (Orange) Sal volatile) carbonate (others: volatile oils of Fe +2 = Green nutmeg & lemon, EtOH) +3 = Yellow/ Orange/ Brown Co +2 + Pink 1B: Coinage Metals Ni +2 = Green Occurrence: Free or in complexes/ chelates (easily recover from ore – Metallurgy) 1A: Alkali Metals Malleable, Conductor of heat and electricity: 3rd: Cu+1, +2 H, Li, Na, K, Rb, Cs, Fr, NH4+ 2nd: Ag+1 Most reactive group (seldom free in nature). Soluble gr 1st: Au +1,+3 Activity, alkalinity: ↑ with atomic number Degree of solvation: ↓ with atomic number Copper (Cu) Valence: +1 Cuprum Cuprous (Cu+1) – readily undergoes disproportionation (Cu+1 Hydrogen (H2) → Cu0 + Cu+2) Water forming – when burned with O2 → H2O Only reddish metal Inflammable air (+) Hemocyanin (respiratory pigment) and cytochrome Lightest element – (1g/mol) oxidase (FeCu) Prep: Lane & Messerschmidt Process (99% pure H2O) Use: Protein precipitant (heavy metal) Isotopes: Protium – most abundant, common and stable isotope Silver (Ag) Deuterium – heavy isotope (D2O Deuterium oxide Argentum, Shining, Bright "heavy water" – Deuterated solvent is used as solvent Fine silver (99.9% pure; too soft) in NMR Spectroscopy) Use: Tritium – radioactive isotope Oligodynamic → germicidal action: ability of certain Industrial uses: heavy metals to inhibit microorganism growth in small Haber Process – (N2 + 3H2 → 2MH3 @ high pressures) concentration production of ammonia Protein precipitant (heavy metal) Oil hydrogenation - production of margarine Balloon inflation - not used anymore Silver Proteinates Medicinal Use % Ag GC gas carrier (also He, N) Mild silver protein (Argyrol) Antiseptic for the eyes 19-23 Strong silver protein ENT germicide 7.5-8.5 Lithium (Li) (Protargol) Lithos (earth, rock Colloidal silver protein General germicide 10-22 (Collargol) lightest metal * Colloidal AgCl/ Lunosol Use: Diuretic (S/E: hypovolemia, hyponatremia) Mood stabilizer (sedative); DOC for Mania (S/E: narrow TI) Gold (Au) Lithium bromide – additive sedative effects Aurum, Shining dawn, King of all metals Lithium carbonate - Widely used in the prophylaxis and 24 karats (purest) treatment of bipolar disorders; last line of therapy for Can be dissolved by: Mania Aqua regia: HCl + HNO3 (3:1) - Li2CO3 capsules - Eskalith® Selenic acid: H2SeO4 – only single acid that can - Li2CO3 tablets - Lithase® dissolve gold - Li2CO3 extended-release tablet - Quilonium-R® Gold preparation – DMARD (RA, Gout); before –“trex” Non-pharmacological use: air-con heat exchanger Aurothioglucose (Solganal®), IM Gold sodium thiomalate (Mypchrysin®), IM Sodium (Na) Auranofin (Ridaura®), PO Natrium (native) Purple of Cassius – Colloidal gold with Stannic hydroxide – Cation of choice for organic medicinal Sn(OH)4 Potassium (K) 2A: Alkaline Earth Metals Kalium (Potash): soluble K+ salts Use: Diuretic, Muscle contractant Be, Mg, Ca, Sr, Ba, Ra Rubidium (Rb) Valence: +2 Spectral line: red; 1861 Beryllium (Be) Cesium (Cs) Most toxic metal (never employed in medicine) Spectral line: blue; 1860 (+) Fluorescent lamp Catalyst in resin polymerization 1st element discovered by use of spectroscope (Kirchoff- Magnesium (Mg) bunsen spectroscope) Lightest of structurally important metals (+) Chlorophyll (photosynthesis), flares Francium (Fr; France) (+) Grignard Reagent (RMgX – Alkyl Mg Halide; Alcohol synthesis) Sources: they come in the form of double salts Module 1 – Inorganic Pharmaceutical Chemistry Page 3 of 12 RJAV 2022