Inorganic Pharmaceutical Chemistry Review PDF
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Cherry Caroline S. Chua, Joanna J. Orejola
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Summary
This review covers inorganic pharmaceutical chemistry topics, including alkali metals, hydrogen, water, and various inorganic compounds. It details characteristics, properties, and uses of these substances in pharmaceuticals and medical applications. Intended for undergraduate study.
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INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 1 Example CHARACTERISTICS INORGANIC PHARMACEUTICAL CHEMISTRY ALKALINE o contain appreciable quantit...
INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 1 Example CHARACTERISTICS INORGANIC PHARMACEUTICAL CHEMISTRY ALKALINE o contain appreciable quantities of Na2SO4, WATER MgSO4 and NaHCO3 REVIEWER CARBONATED o contains CO2 under pressure and usually WATER effervesce on coming to the surface Prepared by Cherry Caroline S. Chua, 11-2012 o contain calcium and magnesium carbonates in Revised by Joanna J. Orejola, 09-2013 solution as bicarbonate o can be natural or artificial GROUP IA (1): ALKALI METALS CHALYBEATE o Contains iron in solution or in suspension WATER o Characterized by its ferruginous taste Possess only one valence electron o Forms ferric hydroxide or ferric oxide upon Very reactive chemically exposure to air Seldom found free in nature LITHIA WATER o Do not contain appreciable quantities of lithium, Lithium, Sodium, and potassium metals are stored under either as carbonate or chloride kerosene→Violent (exothermic, explosive) reaction with water SALINE WATER o Contain relatively high amounts of MgSO4, Hydrogen, H →(Gk. hydro, water; genes, forming – produces water (PURGATIVE Na2SO4 and NaCl when burned with oxygen) WATER) SULFUR WATER o Contains dissolved H2S and deposit S upon Lithium, Li →(Gk. lithos, rock – because it occurs in rocks) exposure to the atmosphere Sodium, Na →(L. sodanum, headache remedy; symbol, L. natrium, SILICEOUS o Water that contain soluble alkali silicates soda) WATER Potassium, K →(L. kalium, potash) Water Hardness→ due to presence of dissolved minerals in water Rubidium, Rb →(L. rubidius, dark red – discovered with the Soft water→Water that does not contain appreciable amounts of spectroscope, its spectrum shows red lines) Ca+2 and Mg+2 ions Cesium, Cs→ (L. caesium, blue – spectral lines are blue) Hard water→Water that contains appreciable quantities of minerals Francium, Fr → (France) Temporary hardness o Contains mainly dissolved calcium and magnesium HYDROGEN, H bicarbonate o Can be removed by boiling (promotes formation of insoluble “Inflammable Air” calcium carbonate) or by addition of lime, Ca(OH)2 Lightest element o Permanent hardness Among the alkali metals, only Hydrogen can exist as a monovalent o Contains mainly dissolved calcium and magnesium sulfate ion (H+) or a monovalent anion (H-) and chloride in water Isotopes: o Cannot be removed by boiling o Protium →Most abundant isotope o Water softening is achieved by the use of ion-exchange resins o Deuterium→ Heavy hydrogen D2O, heavy water Potable Water o Tritium →Radioactive isotope water that is fit to drink Hydrogen, under normal conditions, exist as a diatomic molecule USP Definition: Water that is obtained by distillation, ion exchange, (H2), though this form is not very useful pharmaceutically or reverse osmosis Industrial uses: meets standards for freedom from coliform organisms o Haber process (production of ammonia) water treated to remove insoluble matter through appropriate o Hydrogenation of oils coagulating, settling, and filtering processes; destruction of o Inflating balloons pathogenic microorganisms by aeration, chlorination, or other methods, and improvement of palatability through aeration and WATER, H2O filtration through charcoal Natural Water/Mineral Water water fluoridation contain dissolved minerals (Ca+2, Mg+2, Fe+3, Na+, K+, HCO3-, SO4-2, o Achieved via addition of sodium fluorosilicate Cl-), varying amounts of suspended matter (clay, sand, o For prevention of dental caries microorganisms, fragments of plants and animals), and traces of o Drawback: could cause dental fluorosis (mottling of teeth) dissolved atmospheric gases, ammonia, and metabolic decomposition products Purified Water Not fit for drinking Intended for use as an ingredient of official preparations and in tests and assays unless otherwise specified INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 2 Not for parenteral preparations Not used in treatment of heavy metal poisoning since hypocalcemia rapidly develops HYDROGEN PEROXIDE, H2O2 Agua oxigenada, agua oxenada MONOBASIC SODIUM PHOSPHATE, NaH2PO4 Oxygenated acid, oxygenated water Component of Fleet enema Use: treatment for Vincent’s stomatitis (severe form of gingivitis), as Fleet Enema is composed of Sodium Phosphate and Sodium mouthwash Biphosphate Commercial availability: Saline laxative o 10-volume solution (3% w/v) and 20-volume solution (6% w/v) o Not absorbed from the intestines o Hydrogen Peroxide Topical Solution, USP Systemic and urinary acidifier o 3% w/v stabilized aqueous solution With Methenamine, treatment of cystitis (release of formaldehyde) o 10-volume solution o Hairs of corn, as decoction – used for cystitis o Stabilizer: acetanilide 0.03% Source of phosphorus in hypophosphatemia and TPN Indirectly lowers plasma calcium levels→Excess plasma phosphate LITHIUM, Li interacts with plasma calcium and is transferred to the bone Lithos - “Earth” Used in the treatment of hypercalcemia Lightest metal Pharmacologic action of lithium compounds: DIBASIC SODIUM PHOSPHATE, Na2HPO4 o Mood stabilizer (depressant) Sodium Phosphate, Phosphate of Soda o Diuretic Dibasic phosphate ion is the primary anion in the intracellular fluid Saline laxative LITHIUM BROMIDE, LiBr Antihypercalcemic, as oral solution Combined sedative effects of lithium ion and bromide ion TRIBASIC SODIUM PHOSPHATE, Na3PO4 LITHIUM CARBONATE, Li2CO3 No pharmacologic use Brand names: Eskalith®, Lithase®, Quilonium-R® Used for cleaning glass apparatus Widely used in the prophylaxis and treatment of bipolar disorders and Very alkaline reaction with water (corrosive) mania and in the maintenance treatment of recurrent depression Also used for treatment of mania: SODIUM ACETATE, NaCH3COO o Lithium Citrate Diuretic o Lithium Hydroxide Systemic and urinary alkalizer o Lithium Oral Solution Pharmaceutical necessity used in solutions for hemodialysis and peritoneal dialysis SODIUM, Na Alkalinizing agent for Benedict’s Solution From Latin word “natrium” SODIUM ASCORBATE, NaC6H7O6 Principal extracellular ion Vitamin C supplement Accumulation of too much sodium in the body causes fluid retention Antioxidant Cation of choice for organic medicinals SODIUM BICARBONATE, NaHCO3 CALCIUM DISODIUM EDETATE, C10H12N2Na2 CaO8 Baking Soda Used in antidotal therapy for certain heavy metal poisoning Solvay process (particularly for lead) Bicarbonate ion is the 2nd major anion in the extracellular fluid Does not precipitate hypocalcemia Systemic alkalizer Systemic antacid EDETATE DISODIUM, C10H14N2Na2O8.2H2O o Readily absorbed by the body EDTA Disodium salt o Could cause systemic alkalosis Pharmacologic Use: Chelating agent administered IV in the o Rebound hyperacidity emergency treatment of hypercalcemia Pharmaceutically used as source of carbonation for effervescent Hypocalcemia may occur if the drug is administered too rapidly or to preparations patients who are not initially hypercalcemicLife threatening o Organic acid component: tartaric, citric, ascorbic acid o CO2 enhances palatability of preparation INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 3 Antidote for zinc poisoning (ingestion) Nonpharmaceutical use: Enhance elimination of acidic drugs Rodenticide and insecticide 4 commonly used antacids Hydrofluoric Acid is used in glass etching and causes slow-healing o Sodium Bicarbonate burns (antidote: calcium gluconate) o Calcium Carbonate o Magnesium Hydroxide SODIUM FORMALDEHYDE SULFOXYLATE o Aluminum Hydroxide Best antidote for mercuric chloride poisoning SODIUM BORATE, Na2B4O7 SODIUM GLUCONATE, NaC6H11O7 Borax Electrolyte replenisher Pharmaceutic necessity: alkalinizing agent Gluconate salts: Externally: as eyewash, buffer→Water-softener o less irritating o water soluble SODIUM CARBONATE, Na2CO3 o Acceptors of hydrogen ions produced by metabolic processes Anhydrous – soda ash and act as indirect source of bicarbonate ions Dihydrate – trona Decahydrate – soda crystals, washing soda, sal soda SODIUM HYDROXIDE, NaOH Carbonating agent Caustic soda, lye, sosa, soda lye Very deliquescent→ readily absorb water from the environment and SODIUM CHLORIDE, NaCl readily dissolve in the water that was absorbed Table salt, rock salt, sea salt, solar salt, dendritic salt Saponifying agent→ Manufacture of soaps Chloride is the major extracellular anion o Soft Soap vs. Hard Soap Electrolyte replenisher Corrosive o NSS→ 0.9% w/v NaCl in water Readily attack glass o Ringer’s Solution NaCl, KCl and CaCl2 in water→Isotonic Too alkaline to be of medicinal value→rapidly destroys tissue Solution of Three Chlorides (caustic) o Lactated Ringer’s NaCl, KCl, CaCl2, sodium lactate Pharmaceutical use: →Hartmann’s Solution o alkalinizing agent to form soluble sodium salts of various drugs o Oral rehydration salts→NaCl, glucose, KCl, sodium citrate o Pharmaceutical necessity in preparation of Glycerin Tonicity-adjusting agent Suppositories Condiment Ingestion of solutions of sodium hydroxide causes liquefaction Preservative necrosis/ saponification necrosis (vs. strong acids – coagulative necrosis) SODIUM CITRATE, Na3C6H5O7 In vitro: anticoagulant, forming complex with Ca++ necessary for SODA LIME, NaOH. Ca(OH)2 blood clotting Calx sodica In vivo: Mixture of calcium hydroxide and sodium or potassium hydroxide or o Systemic and urinary alkalizer both o Expectorant Good carbon dioxide absorber for anesthesia machines, oxygen o In vivo (parenteral): blood coagulant therapy, and metabolic tests o Excessive oral administration of citrate salts can have a laxative effect SODIUM HYPOPHOSPHITE, NaHPO2 Best expectorant: water vapor Reducing agent SODIUM FLUORIDE, NaF SODIUM HYPOCHLORITE, NaOCl Anticariogenic agent (1.1%) in dentifrices Household bleach, Chlorox → 4-6% w/w NaOCl in water Excess of fluoride ion causes dental fluorosis (mottling of teeth) Bleaching agent NaMFP (Sodium Monofluoride Phosphate) →also used in Disinfectant (oxidizing property) dentifrices Dakin’s Solution → disinfectant Fluoride ion is toxic and should not be ingested in large amounts Labarraque’s Solution (~2.5%) →disinfectant o Precautions for use in children INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 4 Modified Dakin’s Solution(450-500 mg NaOCl per 100 mL Readily releases oxygen in contact with oxidizable matter solution)→ antiseptic SODIUM POLYMETAPHOSPHATE SODIUM IODIDE, NaI Calgon®, Graham’s salt Iodide is an essential ion necessary for synthesis of triiodothyronine Water-softener and thyroxine detergent Source of iodine o Lack of iodine→ simple or colloid goiter Iodides: expectorant SODIUM POLYSTYRENE SULFONATE action (oral administration) Brand name: Kayexalate expectorant Cation-exchange resin for treatment of hyperkalemia resulting from Pharmaceutical use→ Solubilizer of iodine in iodine-containing kidney failure preparations such as Iodine Tincture and Iodine Solution Protect from moisture and light SODIUM POTASSIUM TARTRATE, NaKC4H4O6. H2O Rochelle Salt, Sal Seginette SODIUM METABISULFITE, Na2S2O5 Saline laxative→ poorly absorbed in the intestine Water-soluble antioxidant→Good reducing agent Sequestering Agent in Fehling’s Solution A combination of sodium bisulfite and sodium metabisulfite in Acidity Regulator in food varying proportions SODIUM SACCHARIN It is the bisulfite of commerce and for all practical purposes Artificial sweetener possesses the same properties as the true bisulfite Antioxidant for drugs which contain phenol or catechol nucleus (e.g: SODIUM STARCH GLYCOLATE phenylephrine HCl, epinephrine HCl solutions) to prevent oxidation Brand name: Explotab to quinones; also in Vitamin C solutions (usually 0.1%)→Solutions Tablet disintegrant must be acid in pH Antimicrobial property: SODIUM SULFATE, Na2SO4. 10H2O o Fermentation industries Glauber’s salt o Preservative and bleach in food Saline laxative→ Sulfate ion poorly absorbed in GIT To prepare water-soluble analogs of water-insoluble drugs (e.g.: menadione sodium bisulfite) SODIUM TARTRATE, Na2C4H4O6 Drawback of sulfites and SO2 → Hypersensitivity reactions in Primary standard for Karl Fischer Reagent used for Water Content susceptible individuals (angioedema, bronchospasm, anaphylaxis) Determination Laxative SODIUM NITRATE, NaNO3 Diuretic Chile saltpeter, salitre NOT converted to bicarbonate inside the body Preservative SODIUM THIOCYANATE, NaSCN SODIUM NITRITE, NaNO2 Hypotensive agent Internally acts as a vasodilator due to relaxation of smooth muscle Also used in cleaners for contact lenses and as antioxidant (can cause lowering of blood pressure) synergist in cosmetic and pharmaceutical preparations Antidote for cyanide poisoning Used for curing meats and fish SODIUM THIOSULFATE, NaS3O3 o Color development Hypochlor, Photographer’s hypo, hypo o Flavor production (with sodium chloride) Sodium hyposulfite (misnomer) o Preservation against bacteria Antidote for cyanide poisoning, in conjunction with sodium nitrite However: carcinogenic Used as volumetric solution in titration Acids decompose thiosulfate to sulfur SODIUM NITROPRUSSIDE, Na2[Fe(CN)5NO]. 2H2O Bases decompose thiosulfate to sulfate Hypotensive agent Prone to bacterial decomposition Removal of chlorine from aqueous solutions SODIUM PERBORATE, NaBO3 Mild disinfectant and deodorant INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 5 MONOSODIUM GLUTAMATE (MSG) Astringent Brand: Ajinomoto Styptic Flavor enhancer Antiperspirant o Imparts a meat flavor to foods (flavor enhancer) Deodorant o Sharpens weaker flavors already present in food without adding any significant taste of their own POTASSIUM BICARBONATE, KHCO3 Causes Chinese Restaurant Syndrome→ some individuals Systemic antacid sensitive to glutamate: light-headedness, headache, uncomfortable Diuretic sense of warmth, difficulty in breathing Electrolyte replenisher May cause hyperkalemia on prolonged use POTASSIUM, K Carbonating agent for Magnesium Citrate Oral Solution, USP “Kalium” Principal intracellular cation POTASSIUM BITARTRATE, KHC4H4O6 Deficiency state → Hypokalemia Cream of tartar, argol, acid potassium tartrate o Due to severe burns, diarrhea, or other causes Occurs in acidulous fruits = grapes o Signs and symptoms: muscle weakness and muscle paralysis Saline laxative Pharmacologic action: Ingredient on baking powder to raise dough o Diuretic o Involved in muscle contraction POTASSIUM BROMIDE, KBr Depressant DIBASIC POTASSIUM PHOSPHATE, K2HPO4 Sedative Potassium Phosphate Used for preparation of samples for IR analysis (pellets) Treatment of hypercalcemia o Favors deposition of calcium and phosphate in the bone POTASSIUM CARBONATE, K2CO3 o A portion is converted to pyrophosphate, a chelator of calcium, Potash, Pearl ash, Salt of tartar, Salt of wormwood the complex excreted in the urine Pharmaceutical necessity (basic property) o High plasma phosphate levels decrease calcitriol levels and Carbonating agent decrease absorption of calcium Used in conjunction with monobasic salt for potassium or phosphate POTASSIUM CHLORATE, KClO3 deficiency Deodorant action due to oxidizing capability Reagent for various buffers and parenteral fluids No longer used as laxative POTASSIUM CHLORIDE, KCl Potassium salt of choice for potassium replenishment MONOBASIC POTASSIUM PHOSPHATE, KH2PO4 Electrolyte replenisher Sorensen’s Potassium Phosphate Component of Ringer’s Injection For treatment of hypercalcemia →Used in conjunction with the As IV injection, administered as drip, not push →Muscles and heart dibasic salt contracts Urinary acidifier Used in lethal injection o For treatment of calcific kidney stones (nephrolithiasis) Component of Ringer’s and Darrow’s Solution (composition: KCl, →decrease in free calcium excretion in the urine decreases NaCl and sodium lactate) stone formation and acidification of urine and free High local concentrations in the GIT can lead to ulceration pyrophosphate ion favor dissolution of stones o Can cause diarrhea POTASSIUM CITRATE, K3C6H5O7 Systemic alkalizer POTASSIUM ACETATE, KCH3COO Osmotic diuretic Urinary and systemic alkalizer POTASSIUM GLUCONATE, KC6H11O7 Diuretic Electrolyte replenisher for hypokalemic states Antacid Less irritating compared to potassium chloride POTASSIUM ALUM, AlK(SO4)2.12H2O Tawas INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 6 POTASSIUM HYDROXIDE, KOH Dark purple or almost black crystals or granular powder, almost Caustic potash, lye potash opaque by transmitted light and with a blue metallic luster by Strong base; very corrosive reflected light Saponifying agent Strong oxidizing agent Used for manufacture of soft soap Local anti-infective, antiseptic, deodorant Used as volumetric solution in titrimetry POTASSIUM IODIDE, KI Iodide salt of choice POTASSIUM SORBATE, KC6H7O2 Expectorant Pharmaceutical aid → preservative (0.2%) Solubilizer for iodine Antimicrobial → control growth of yeasts and mold in enteral Prolonged use could lead to hypothyroidism formula, foods, and cosmetic preparations Excessive amounts could lead to Iodism Relatively ineffective above pH 6.5 o a condition produced by excessive amounts of iodine in the body POTASSIUM THIOCYANATE, KSCN o characterized by increased lacrimation and salivation, rhinitis, Hypotensive agent weakness, and skin eruption Used for prevention of goiter SULFURATED POTASH, K2Sx.. K2S2O3 o Iodine, in the form of iodide, is a necessary nutrient for the Liver of sulfur, hepar sulfuris, potassa sulfurata synthesis of thyroid hormones o Irregular, liver brown pieces rapidly changing to greenish- For treatment of hyperthyroidism yellow on exposure to air To prepare for thyroid surgery (with anti-thyroid medications) o Possess odor of hydrogen sulfide o As saturated solution Used in preparation of White Lotion To protect the thyroid in cases of radiation emergency Reacts with zinc sulfate to precipitate zinc sulfide o Tablets, oral solution o Source of sulfide ion in preparation of White Lotion, USP used Drug of choice for cutaneous lymphatic sporotrichosis (SSKI 1g/mL) in dermatological practice as: Used for prevention of goiter Astringent, protective, mild antimicrobial and antifungal Iodine, in the form of iodide, is a necessary nutrient for the Treatment of parasitic diseases of the skin synthesis of thyroid hormones For treatment of hyperthyroidism AMMONIA AND AMMONIUM COMPOUNDS To prepare for thyroid surgery (with antithyroid medications) Ammonium ion is a hypothetical alkali metal As saturated solution Pseudo-alkali metal ion To protect the thyroid in cases of radiation emergency Generally, ammonium compounds are very water soluble Tablets, oral solution BUT: ammonium hydroxide is a weak base as compared to alkali Drug of choice for cutaneous lymphatic sporotrichosis (SSKI 1g/mL) hydroxides which are strong bases Pharmacologic action: POTASSIUM METABISULFITE, K2S2O5 o Osmotic diuretic Antioxidant o Buffer component Can trigger allergic reactions in hypersensitive individuals o Expectorant POTASSIUM NITRATE, KNO3 AMMONIA, NH3 Saltpeter, salitre, salt prunelle Synthesized via Haber Process Used as a meat preservative Involves combination of hydrogen and nitrogen gas at high Tooth-desensitizing agent pressures to produce ammonia Used in pharmacy in dilute form as respiratory stimulant POTASSIUM PERCHLORATE,KClO4 Household ammonia: 10% NH3 and is known as 16o ammonia Strong oxidizing agent (degrees Baumé) Anti-thyroid agent (for the treatment of hyperthyroidism) As blocking agent for I-131 STRONG AMMONIA SOLUTION Stronger ammonia water, stronger ammonium hydroxide solution, POTASSIUM PERMANGANATE, KMnO4 spirit of Hartshorn Mineral chameleon Prepared by Haber process: N2 + 3H2 2NH3 + heat o Contains 27% to 31% w/w of NH3 INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 7 o Very pungent and characteristic odor o Spirit of sal volatile, Spirit of Hartshorn o Strongly alkaline to litmus even when diluted o Used as a respiratory stimulant in cases of hysterical syncope o On exposure to air it loses ammonia rapidly o Solution is caustic and vapors irritating (avoid inhalation) AMMONIUM CHLORIDE, NH4Cl o Cool container well before opening, cover the closure with Muriate of Hartshorn, sal ammoniac cloth while opening Diuretic Expectorant AMMONIA WATER Systemic acidifier Dilute Ammonia Solution Urinary acidifier o Contains 9.5-10.5% w/w of NH3 o Used as reflex respiratory stimulant AMMONIUM FERRIC CITRATE o To neutralize insect stings and jellyfish stings of Portuguese hematinic man-of-war AMMONIUM IODIDE, NH4I AROMATIC AMMONIA SPIRIT expectorant Respiratory stimulant Components: Ammonium Carbonate, NF and Strong Ammonia AMMONIUM PHOSPHATE, (NH4)2HPO4 Solution, NF Formerly used as diuretic Components: Ammonium Carbonate, NF and Strong Ammonia Used as buffering agent in pharmaceutical preparations Solution, NF, volatile oils (nutmeg and lemon) and ethanol AMMONIATED MERCURY, HgNH2Cl GROUP IB (11): COINAGE METALS White precipitate Copper Topical anti-infective Silver Gold AMMONIUM ACETATE, Al(CH3COO3)3 Spirit of Mindererus COPPER AND COPPER COMPOUNDS Buffer Component COPPER, Cu Cuprum AMMONIUM ALUM, Al(NH4)(SO4)2 12H2O Only reddish colored metal Depressant Third most malleable metal Tawas Excellent conductor of heat (surpassed only by silver and gold) and Astringent electricity (surpassed by silver) Styptic Forms two series of salts Antiperspirant o Cuprous ion (Cu+1) Deodorant Readily undergo disproportionation Water insoluble AMMONIUM BROMIDE, NH4Br All are white except Cu2S and Cu2O Depressant o Cupric ion (Cu+2) Sedative Generally blue in solution Important alloys AMMONIUM CARBONATE, (NH4)2 CO3 o Bronze → Cu and Sn Ammonia crystal, sal volatile, ammonium sesquicarbonate, o Brass → Cu and Zn Preston’s salt, Hartshorn, baker’s ammonia Present on hemocyanin and cytochrome oxidase Composed of ammonium bicarbonate and ammonium carbamate Respiratory proteins – chromoproteins (NH2COONH4) Color is due to copper Readily converted to ammonium carbonate in the presence of Pharmacologic action: ammonia o Protein precipitant (heavy metal) Expectorant o Enhances utilization of iron Respiratory stimulant – decomposes to NH3 and CO2 Toxicity: Wilson’s Disease Source of ammonia for “smelling salts” o Accumulation of too much copper in the body Used in the preparation of Aromatic Ammonia Spirit o Antidote: Penicillamine (Cuprimine) INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 8 COPPER ACETO-ARSENATE GOLD AND GOLD COMPOUNDS Paris green GOLD, Au Insecticide “Aurum” King of all metals CUPRIC SULFATE, CuSO4. 5H2O Most malleable metal Blue vitriol, blue stone, Roman vitriol, Salzburg vitriol Best conductor of electricity Component of Benedict’s solution, Fehling’s solution and Barfoed’s Precious metal – expensive solution→Test for reducing substances Very soft and ductile Bordeaux Mixture→Cupric sulfate and lime (CaO) Can only be dissolved by: o Algaecide and fungicide in swimming pools o Aqua Regia (3 parts HCl: 1 part HNO3) Enhance utilization of iron o Selenic Acid Antidote for phosphorus poisoning Purple of Cassius→Colloidal gold with stannic hydroxide Toxicity: Gold dermatitis SILVER AND SILVER COMPOUNDS o Antidote: BAL/ Dimercaprol SILVER, Ag “Argentum” GOLD COMPOUNDS Very soft, ductile and malleable metal Used for treatment of rheumatoid arthritis Fine silver 99.9% pure – too soft Aurothioglucose Usually alloyed to give strength while preserving ductility and Gold Sodium Thiomalate beauty of the metal Auranofin→ p.o. o Sterling Silver (92.5% Ag, 7.5% Cu, usually) Pharmacologic action: o Protein precipitant (heavy metal) GROUP IIA (2): ALKALINE EARTH METALS o Oligodynamic action 2 valence electrons Toxicity : Argyria Form divalent ions o Darkening of skin due to chronic use of silver preparations Selected General Reactions of Group 2A Elements: o Antidote: NSS Equations Reaction M + 2H2O → M(OH)2 + H2↑ Be probably reacts with SILVER IODIDE, AgI steam germicide Mg reacts with hot water Ca, Sr and Ba reacts rapidly SILVER NITRATE, AgNO3 with cold water Lunar caustic M + 2HCl → MCl2 + H2↑ All metals react with acids, Water soluble salt of silver liberating H2 Lapiz infernularis (caustic pencil) Component of indelible ink Be + 4NaOH → Be is amphoteric Used for treatment of warts Na2[Be(OH)4] + 2Na+ Only Be reacts with NaOH 1% ophthalmic solution: prophylaxis for gonorrhea ophthalmia 2M + O2 → 2MO Normal oxide formed by all neonatorum (can cause blindness to the newborn) group members Tollen’s Reagent (ammoniacal silver nitrate) Ba + O2 (excess)→ BaO2 Tendency and stability in o Silver mirror test (presence of reducing substances, such as forming peroxides increases aldehydes) with increasing atomic number Ba forms peroxides SILVER PROTEINATES M + H2 → MH2 All metals from hydrides Silver Proteinate Medicinal Use % Ag 3M + N2 → M3N2 All form nitrides at high Mild Silver Protein (Argyrol) Antiseptic for eyes 19-23 temperatures Strong Silver Protein (Protargol) Antiseptic for ears and 7.5-8.5 throat BERYLLIUM, Be Colloidal Silver Protein(Collargol) General germicide 18-22 Not used pharmaceutically Most toxic metal INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 9 MAGNESIUM AND MAGNESIUM COMPOUNDS MAGNESIUM TRISILICATE, 2MgO. 3SiO2. H2O MAGNESIUM, Mg Antacid Lightest of all structurally important metals Advantages: Natural sources: o Can protect ulcers by forming a protective coating on the o Silicate – talc, asbestos stomach o Carbonate – magnesite, dolomite o Gelatinous consistency provides prolonged antacid effect o Sulfate – kieserite Mg2+: CALCIUM AND CALCIUM COMPOUNDS o 2nd most abundant intracellular cation o Found in chlorophyll CALCIUM, Ca o Grignard Reagent (RMgX) used for synthesis of alcohols Calcium ion is the second most abundant extracellular cation o Pharmacologic action: Sources: Cathartic o Dolomite MgCO3CaCO3 Depressant action o Fluorite CaF Natural calcium-channel blocker o Gypsum CaSO4 o Phosphate Rock Ca3(PO4)2 MAGNESIUM CARBONATE, MgCO3 o Apatite CaF and Ca3(PO4)2 Magnesia 2 forms: light and heavy Pharmacologic action: Antacid o Blood coagulation factor Laxative o needed for the conversion of prothrombin to thrombin o Release of neurotransmitters (norepinephrine) MAGNESIUM CITRATE, Mg3(C6H5O7)2 o Muscle contraction Lemonada purgante, purgative lemon o Structural material of bones and teeth Saline cathartic Vitamin D is required for maximum absorption of Calcium MAGNESIUM HYDROXIDE, Mg(OH)2 Vitamin C = Fe absorption Milk of Magnesia, Magnesia Magma Vitamin E = Se absorption Antacid Side effect: can cause diarrhea Calcium deficiency: o Osteomalacia (adults) MAGNESIUM OXIDE, MgO o Rickets (children) Calcined Magnesia o Osteoporosis Antacid Laxative CALCIUM BROMIDE, CaBr2 Component of Universal Antidote→ MgO, activated charcoal, tannic Sedative/depressant acid Not effective for cyanide and kerosene poisoning CALCIUM CARBIDE, CaC2 Kalburo MAGNESIUM SULFATE, MgSO4 Epsom salt CALCIUM CARBONATE, CaCO3 Oral administration: cathartic Two important forms: Intramuscular administration: anticonvulsant o Precipitated Calcium Carbonate Commercially produced by chemical means HYDRATED MAGNESIUM TRISILICATE (TALC), 3MgO.4SiO2.H2O o Prepared Calcium Carbonate Soapstone, French chalk Native, calcium carbonate purified by elutriation Softest mineral Dusting powder 2 crystal forms: Clarifying agent o Aragonite Filtering aid o Calcite → natural birefringent crystal Adsorbent INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 10 Iceland Spar→very pure form of calcite o inhalation Polarimeters o ingestion of water-soluble barium compounds: Optical birefringence o Muscle stimulating action Antacid o Antidote: Magnesium Sulfate Can cause rebound hyperacidity BARIUM HYDROXIDE, Ba(OH)2.8H2O CALCIUM CHLORIDE, CaCl2 Component of Barium Hydroxide Lime Muriate of lime Similar to soda lime Electrolyte replenisher in hypocalcemic states CO2 absorber Component of Ringer’s solution A saturated solution of barium hydroxide in water is known as baryta water CALCIUM GLUCONATE, C12H22CaO14 Most commonly used calcium salt as electrolyte replenisher BARIUM SULFATE, BaSO4 Less irritating than Calcium Chloride Radiopaque for imaging of GIT Can cause constipation CALCIUM HYDROXIDE, Ca(OH)2 Slaked lime, milk of lime, calcium hydrate RADIUM Saponifying agent RADIUM,Ra Discovered by Marie Curie CALCIUM HYPOCHLORITE, Ca(OCl)2 Radioactive Bleaching agent Old unit for radioactivity: Curie Disinfectant SI unit: Becquerel Diagnostic purposes CALCIUM OXIDE, CaO Treatment of certain types of cancers Lime, Quicklime, Calx, Apog, Burnt Lime, Calx Usta Component of Bordeaux mixture → insecticide GROUP IIB (12):VOLATILE METALS/VOLATILE ELEMENTS Zinc Family CALCIUM PHOSPHATE, Ca3(PO4)2 Metals have relatively low melting points Bone ash Zinc Antacid Cadmium Major component of bone Mercury Product of cremation ZINC AND ZINC COMPOUNDS CALCIUM SULFATE, (CaSO4)2.H2O or CaSO4.1/2H2O ZINC, Zn Plaster of Paris Present in insulin Used in surgical cast Container for batteries and dry cells CaSO4 2H2O Protective coating in galvanized iron Gypsum, terra alba Pharmacologic properties: Dentifrice o Astringent o Antiseptic STRONTIUM AND STRONTIUM COMPOUNDS o Antiperspirant STRONTIUM, Sr o Deodorant Imparts crimson red to a nonluminous flame o similar to Aluminum Deficiency state: Parakeratosis STRONTIUM CHLORIDE, SrCl2 o Skin appears to be scaly, thickened and inflamed Tooth desensitizing agent Important in immune system Active ingredient in Sensodyne toothpaste Deficiency state leads to impaired immunity BARIUM AND BARIUM COMPOUNDS Antidote for Zn2+ poisoning: Sodium Bicarbonate BARIUM, Ba “heavy” ZINC CHLORIDE, ZnCl2 Toxicity: Baritosis Butter of Zinc Burnett’s Disinfecting Fluid INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 11 Antiseptic found in mouthwashes CADMIUM SULFIDE, CdS Dentin desensitizer Only yellow sulfide Antiseborrheic agent (for dandruff) ZINC OXIDE, ZnO Capsebon Zinc White Component of Lassar’s Paste CADMIUM SULFATE, CdSO4 mild antiseptic Ophthalmic antiseptic Astringent Topical protectant MERCURY AND MERCURY COIMPOUNDS Toxicity: Metal Fume Fever MERCURY, Hg o occupational disease from inhalation of ZnO fumes Hydrargyrum, quicksilver, asoge ZnO heated with CoO → Rinman’s Green (CoZnO2) Forms two series of salts: Thenard’s Blue → Cobalt metaaluminate o Mercurous, Hg22+ →More difficult to absorb o Relatively less toxic compared to Hg+2 ZINC PEROXIDE, ZnO2 o Mercuric (Hg2+) Antiseptic Source→Cinnabar (Aethrop’s mineral), - HgS Properties similar to that of hydrogen peroxide Encountered in thermometers, amalgams Release of nascent oxygen provides powerful oxidizing action Toxicity : Minamata Disease Signs and symptoms HYDRATED ZINC SILICATE o Metallic taste, thirst, soreness of throat, salivation, sore gums, Natural calamine bloody diarrhea, severe gastric pain, vomiting (ingestion of prepared calamine→ ZnO with traces of ferric oxide as impurity inorganic Hg salts) o Acute poisoning→Hg+2: severe vomiting, damage to ZINC SULFATE, ZnSO4 intestinal mucosa, diuresis, additional renal damage White vitriol o Chronic poisoning→Behavioral and personality changes, Used as ophthalmic astringent decreased visual acuity, tremors, insomnia, ataxia o 0.25% aqueous solution is the only FDA-approved OTC o Mad hatter’s disease ophthalmic astringent Hg compounds were used to convert fur to felt Used in preparation of White Lotion Tremors, behavioral changes in makers of felt hats o Sulfurated potash and zinc sulfate (1900’s) o Active ingredient in White Lotion: ZnS Toxic Forms o Scabicide, topical anti-infective o Hg+2 > Hg2+2 > Hgo o Organic mercury more toxic than inorganic mercury ZINC-EUGENOL CEMENT (methylmercury) Dental protective o Organic mercury toxicity: Source of eugenol: clove oil Brain damage Numbness CADMIUM AND CADMIUM COMPOUNDS Loss of vision Deafness CADMIUM, Cd Madness Pharmacologic action of water-soluble compounds→ Astringent Death Heavy metal o Elemental and methylmercury → CNS Very poisonous o Mercury vapor → pulmonary irritant Toxicity: Itai-itai disease (Japan) o Methylmercury → teratogenic Source of cadmium: cigarette smoking o Inorganic mercury salts – corrosive to skin, eyes, GIT, Antidote: BAL/ Dimercaprol nephrotoxic Cadmium has high affinity for metallothioneins (stress proteins) o Chronic inhalation of Hg vapor Tremor, neuropsychiatric disturbances CADMIUM CHLORIDE, CdCl2 Gingivostomatitis Emetic Erethism Used for tinea infections Mood changes INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 12 Acrodynia (children)→Pain in extremities, pinkish BORON AND BORON COMPOUNDS discoloration and desquamation (“pink disease”), BORIC ACID, H3BO3 hypertension, profuse sweating, anorexia, insomnia, Sal sedativum Hombergi, Boracic acid, orthoboric acid irritability or apathy, rash Toxic by ingestion or dermal absorption Mechanism of Toxicity o Boiled lobster appearance of skin o Cumulative poisons o Reddish-orange color of skin o Once absorbed, Hg+2 concentrates in kidneys Eyewash (2%) – antiseptic property o Combine with –SH groups of protein leading to inactivation Tonicity adjusting agent (generally for heavy metals) Buffer component Antidotes o Standard pH buffer pH 8-10: Alkaline Borate Buffer o Sodium Formaldehyde Sulfoxylate, NF o Pharmaceutical buffer systems: Best antidote for Hg poisoning, especially Hg2+ Feldman’s (pH 7-8.2) Reduces Hg+2 to Hg2+2, less soluble Atkins and Pantin (pH 7.6-11) – Borate buffer system o Penicillamine (Cuprimine®) Gifford’s (pH 6-7.8) For elemental Hg Sorensen’s (pH 5.9-8) – Phosphate buffer system o Dimercaprol (BAL) o Borate buffers are used in ophthalmic and nasal solutions and not used for poisoning with metallic and organic mercury external preparations (NOT for parenteral preparations) for inorganic Hg salts only o Limitation of phosphate buffers: formation of precipitate with o DMSA (Succimer) – water-soluble analog of BAL certain metal ions (Ag, Zn, Al) Chelating agents For all types of mercury posioning SODIUM BORATE, Na2B4O7.10H2O May redistribute Hg to brain from other tissue Sodium tetraborate decahydrate Pharmacologic action Borax o Diuretic, useful for cardiac edema Dobell’s Solution o Antiseptic – protein precipitant action o aqueous solution of sodium borate, sodium bicarbonate, o Antisyphilitic phenol, and glycerol o Cathartic o used as an astringent or antiseptic wash for the throat and o Parasiticide and fungicide nose MERCUROUS CHLORIDE, Hg2Cl2 ALUMINUM AND ALUMINUM COMPOUNDS Calomel ALUMINUM, Al Cathartic Most abundant metal Active ingredient in Ly-Na 3rd most abundant element Abrasive MERCURIC CHLORIDE, HgCl2 Toxicity (inhalation)→ Shaver’s Disease Corrosive sublimate o Neurotoxin (brain) disinfectant o Cause Alzheimer’s disease in elderly Source→Cryolite 3NaFAlF3 MERCURIC IODIDE, HgI2 Treatment of syphilis ALUMINUM CHLORIDE, AlCl3. 6H2O KI and HgI2 → Mayer’s reagent Astringent o most sensitive alkaloidal reagent Antiseptic o White precipitate (+ result) Antiperspirant Deodorant MERCURIC OXIDE, HgO Yellow precipitate ALUMINUM HYDROXIDE, Al(OH)3 Ophthalmic anti-infective Gastric antacid Brand names: Amphojel, Cremalin GROUP IIIA (13) – BORON/ALUMINUM FAMILY Side effects: Mg has a diagonal relationship with aluminium o Constipation o Can interfere with absorption of phosphates INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 13 Maalox GROUP IVA (14) – CARBON FAMILY o Combination of Mg(OH)2 and Al(OH)3 Nonmetallic in character o Counteract side effects of one another CARBON AND CARBON COMPOUNDS ALUMINUM PHOSPHATE, AlPO4 CARBON, C Gastric antacid Exclusively nonmetallic Brand name: Phosphagel Only element which can form multiple bonds with itself Advantage over Al(OH)3→Does not interfere with phosphate CATENATION→ Chain-formation absorption 2 allotropic modifications of Carbon: o Crystalline ALUMINUM CARBONATE, Al2(PO4)3 Diamond (tetrahedral) Treatment of phosphatic calculi → Promotes elimination of Graphite (planar phosphate via fecal route o Amorphous Coal and anthracite ALUM Activated Charcoal Tawas o Residue from destructive distillation of various organic Ammonium Alum and Potassium Alum materials treated to increase its adsorptive power Antiperspirant o Official in the USP: fine form Astringent o Used as adsorbent (poisoning by ingestion) Deodorant Effective for alkaloidal poisons Ineffective against cyanide and kerosene ALUMINUM OXIDE, Al2O3 o Treatment of diarrhea Alumina Treatment of silicosis CARBON DIOXIDE, CO2 Carbonic acid gas ALUMINUM SILICATES Most potent respiratory stimulant Bentonite Stored in GRAY containers o Soapclay, mineral soap Used for treatment of persistent hiccups o Native colloidal hydrated aluminum silicate Toxicity through suffocation o Bentonite Magma Dry ice→ solid form 5% suspension in water o Used as refrigerant Suspending agent o For treatment of acne, warts, corns and eczema Kaolin CARBON MONOXIDE, CO o China clay Colorless, odorless, tasteless gas o Native hydrated aluminum silicate Systemic poison o Adsorbent→ Treatment of mild diarrhea Mechanism of Action: binds to hemoglobin of blood leading to o Demulcent hypoxia CO has higher affinity for hemoglobin compared to oxygen gas Pumice Treatment: o Complex silicate of aluminum, sodium and potassium o 100% Oxygen→inhalation o Volcanic origin o Artificial Air→80% He and 20% O2 o Dental abrasive o CO2-O2 mixture Disadvantage: too abrasive for daily use o Hyperbaric Oxygen GALLIUM SILICON AND SILICON COMPOUNDS Melts at near body temperature Substitute for mercury in the manufacture of arc lamps SILICON, Si Treatment of cancer-related hypercalcemia by binding with Second most abundant element transferrin INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 14 SILICON DIOXIDE, SiO2 Vs. Sodium Fluoride → at least 4 applications\Stannous Fluoride → Silica only one application Inert BUT: solutions should be freshly prepared Very abundant in nature Glass is made up of silica and other additives STANNOUS PEROXIDE, SnO Causative agent of silicosis Germicide against Staphylococcal organisms o Signs and symptoms similar to TB o Haemoptysis – blood in sputum LEAD AND LEAD COMPOUNDS o Silica becomes deposited in the lungs --- irritation LEAD, Pb o Alumina forms a coat with silica particles (antidote “Plumbum” Glass Protein precipitant (heavy metal) Pure silica fused with Effect Forms two series of salts: sodium carbonate o Plumbous (Pb+2) With MnO2 Mask blue green color of iron usually present o Plumbic (Pb+4) in glass Poisoning: Plumbism/ Saturnism With Boron (as borate) Decrease coefficient of expansion of glass o Automobile exhaust With Potassium Render glass brown with light-resistant o Canned foods o Old lead pipes property→ amber-colored glass o Paints containing lead With Lead Increase refractive index of glass o Diagnosis: foot drop/wrist drop Rare Earths Selectively absorb light of certain o Most serious effect→ Lead encephalopathy wavelengths Memory loss Irritability Purified Siliceous Earth Clumsiness o Adsorbent Projectile vomiting o Filtering aid o Clarifying agent LEAD ACETATE, Pb(CH3COO3)2 Sugar of Lead Silicates Astringent o Magnesium trisilicate Used for the preparation of Lead Subacetate Solution o Aluminum silicates → Bentonite, Pumice, Kaolin o Attapulgite → Diatabs, Polymagma, Quintess LEADSUBACETATE, Pb(CH3COO3)2 o Mg5(Si8O20)(OH)28H2O Pb(CH3COO3)2 + PbO o Adsorbent → used for diarrhea Goulard’s Extract Antiseptic Simethicone Astringent o Polymer of dimethylsiloxane o Antiflatulent GROUP IVB (4) – TITANIUM FAMILY o Antifoaming agent TITANIUM AND TITANIUM COMPOUNDS TIN AND TIN COMPOUNDS TITANIUM, Ti TIN, Sn Titans “Stannum” o Sons of the Earth Used in production of cans o Chemically: powerful reducing agent two series of salts: o Stannous (Sn+2) TITANIUM DIOXIDE, TiO2 o Stannic (Sn+4) Solar ray protectant w/ high refractive index→Sunblock White pigment o High coverage area STANNOUS FLUORIDE, SnF2 o Opacifying agent Anticariogenic agent\ o White capsules INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 15 o Pilocarpine Ocusert System (for glaucoma) PHOSPHORUS o Provides white background for easy visibility PHOSPHORUS, P ZIRCONCIUM AND ZIRCONIUM COMPOUNDS Light- carrier ZIRCONIUM, Zr “St. Elmo’s Fire” Similar to Aluminum Essential constituent of protoplasm, nervous tissue and bones Antiperspirant Three main allotropic forms: Deodorant o White Phosphorus Forms: Colorless or white solid with waxy appearance o Aluminum Zirconium Trichlorohydrate Darkens on exposure to light o Aluminum Zirconium Tetrachlorohydrex Gly Sometimes called Yellow Phosphorus, color due to o Aluminum Zirconium Tetrachlorohydrex PG impurities o Aluminum Zirconium Tetrachlorohydrex PEG Stored under water→ handled using forceps Zirconium salts are are known to cause skin granuloma When exposed to air in the dark, it emits a greenish light Use of antiperspirants/deodorants have been linked to breast and gives off white fumes with garlicky odor cancer→ no clear scientific evidence Uses: rat poison Use in aerosols prohibited → pulmonary granuloma VERY POISONOUS! o Acute Ingestion: Garlic odor of breath, luminous ZIRCONIUM OXIDE, ZrO vomitus, severe GI irritation, bloody diarrhea, liver Former official compound damage →general protoplasmic poison Antiperspirant o Chronic Poisoning: bony necrosis, esp. the mandible Treatment of athlete’s foot (“phossy jaw”) o Black Phosphorus ZIRCONIUM CARBONATE, ZrCO3 Resembles graphite in texture Former official compound Produced from white P under high pressures Antiperspirant Stable in air Treatment of athlete’s foot Does not catch fire spontaneously o Red Phosphorus GROUP VA (15) – NITROGEN FAMILY Appears as red to violet powder Properties of red P are intermediate between those of NITROGEN AND NITROGEN COMPOUNDS black and white P NITROGEN, N2 Insoluble in organic solvents (vs. White P which is soluble Exists as a diatomic molecule in ordinary conditions in certain org. solvents) “without life” Less chemically active compared to White P Synonyms: Azote, Mephitic Air Relatively nontoxic unless it contains White P as impurity Provides an inert atmosphere for readily oxidizable pharmaceuticals Uses: safety matches, pyrotechnics Used as a carrier gas in GC Phosphates→ Of physiologic and medicinal importance Stored in BLACK containers Liquid nitrogen: ARSENIC AND ARSENIC COMPOUNDS o Used as a refrigerant ARSENIC, As o Cryogenic preservation Lewisite metal Salvarsan/ Compound 606/ Arsphenamine→ First anti-syphilis NITRATES, NO3-; NITRITES, NO2- drug by Paul Ehrlich Used as preservatives Paris Green – cupric aceto-arsenite NO3- NO2- N-nitrosoamines (carcinogenic) o Rodenticide, insecticide, pigment, blue colorant for fireworks o Made by combining cupric sulfate and arsenic trioxide NITROUS OXIDE, N2O o Cu(C2H3O2)2·3Cu(AsO2)2 Laughing gas, sweet air Scheele’s Green – cupric hydrogen arsenite Inhalatory anesthetic Fowler’s Solution – 1% potassium arsenite solution (KAsO2) Stored in BLUE containers o Antileukemic (before) Donovan’s Solution – arsenic (III) iodide solution INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 16 o For trypanosome infections, rheumatism, arthritis, malaria, TB, BISMUTH AND BISMUTH COMPOUNDS diabetes (before) BISMUTH, Bi Acute poisoning: “beautiful meadow” o Digestive problems – vomiting, abdominal pains, diarrhea Astringent accompanied by bleeding Antiseptic o Mees lines – characteristic white lines on nails Protectant o Hair loss Bismuth compounds are poisonous Chronic poisoning: Arsenicosis Cause black stools --- combination with sulfide ion o Smelters, patients treated with arsenicals, drinking water with Antidote: Dimercaprol high levels of arsenic o cancer BISMUTH SUBNITRATE, Bi(OH)2NO3 Antidote: BAL (Dimercaprol) Used as antacid, with astringent and antiseptic properties General protoplasmic poison o Arsenious ion (As+3): BISMUTH HYDROXIDE, Bi(OH)3 High affinity for –SH compounds Milk of Bismuth→ bismuth hydroxide and bismuth subcarbonate in Trivalent arsenic more toxic than pentavalent arsenic suspension in water o Toxic to all types of cells o Prepared from Bismuth subnitrate, nitric acid, ammonium Napoleon Bonaparte→Arsenic detected on hair strand carbonate, strong ammonia solution, and purified water o Internal protective for gastric ulcers ARSENIC TRIOXIDE, As2O3 o Bismuth salts inhibit growth of H. pylori Synonyms: arsenious oxide, white arsenic, arsenic (III) oxide, arsenicum album BISMUTH CITRATE Amphoteric oxide Colloidal bismuth subcitrate used in tx of PUD Used as a wood preservative Primary standard in titrimetric analysis BISMUTH SUBCARBONATE Trisenox – used as treatment for leukemia that is not responsive to first line agents→ Induces cancer cells to undergo apoptosis BISMUTH SUBGALLATE ANTIMONY AND ANTIMONY COMPOUNDS BISMUTH SUBSALICYLATE (“PINK BISMUTH”) ANTIMONY, Sb Active ingredient in Pepto-Bismol and Kaopectate “Stibium” Anti-inflammatory, bactericidal, antacid Antimony glance Bismuth Subsalicylate Magma o Most important source of antimony o Sb2S3 VANADIUM o Red-orange in color Insulin-mimetic effect (vanadate, vanadyl ion, coordination Pharmacologic action of water-soluble compounds: compounds) o Astringent Drawback: toxicity of the metal o Emetic o Expectorant GROUP VB (5) o Anthelmintic Kills and expels intestinal worms TANTALUM Vs. vermifuge→ only expels worms Unaffected by body fluids → inert Sheet form → surgical repair of bones ANTIMONY POTASSIUM TARTRATE, C8H4K2O12Sb2.3H2O Tartar emetic GROUP VIA (16): CHALCOGENS (OXYGEN FAMILY) Brown mixture o Emetic OXYGEN AND OXYGEN COMPOUNDS o Expectorant OXYGEN, O2 o For treatment of schistosomiasis (liver fluke) Dephlogisticated air, Empyreal air, “Yne” Schistosoma japonicum→ requires 2 hosts: snails and humans Exists as a diatomic molecule under ordinary conditions Consists of 1/5 of air, by weight (in free form) INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 17 Consists of 7/8, by weight, of water and in minerals (in combined o At equilibrium point (96oC): β-Sulfur (monoclinic sulfur) state) becomes the stable form Obtained industrially by fractional distillation of liquid air Occurs in free state and in combination, mainly as sulfides and Three allotropes: sulfates o Nascent→[O] Constitutes 0.05% of the crust of the Earth o Atmospheric/ molecular→O2 Pharmaceutical Sulfur o Ozone→O3 PRECIPITATED SUBLIMED SULFUR WASHED SULFUR Employed as a therapeutic gas in the treatment of conditions SULFUR involving hypoxia Milk of Sulfur; Lac Flowers of Sulfur Stored in GREEN containers sulfur Very active chemically Made by boiling Sulfur Made by treating o Combines directly with elements except Hg, Ag, Au and with Lime and Sublimed Sulfur with members of the Pt family precipitating the Ammonia to dissolve o Second most electronegative element (vs. fluorine) filtered solution with impurities, particularly o Oxides (-2 oxidation state) HCl arsenic and to remove Metallic traces of acid Nonmetallic Very fine, pale Fine, yellow, Fine, yellow crystalline Amphoteric yellow, amorphous or crystalline powder, powder, with faint odor microcrystalline with faint odor and and taste HYDROGEN PEROXIDE, H2O2 powder, odorless and taste Oxidation state of oxygen is -1 tasteless Good oxidizing and reducing agent Readily dissolves in Slowly and usually Slowly and usually Pure solutions are stable carbon disulfide incompletely incompletely soluble Commercial solutions are stabilized by acetanilide and addition of soluble in carbon in carbon disulfide acid (e.g., H3PO4) disulfide Commonly available in 3% and 6% solution Used in ointments Used as cathartic Reagent: 30% solution and lotions 30% Solution o Hydrogen Peroxide Concentrate, USP Used as scabicide --- fungicidal action o Disinfectant, powerful oxidant Keratolytic effect 3% Solution (10-volume solution) Stimulant cathartic o Hydrogen Peroxide Topical Solution, USP Stimulates hair growth o Antiseptic (oxidizing germicide) Depilatory – as thioglycollate 6% Solution (20-volume solution) Fumigant – SO2 o Hair bleach Antiseborrheic agent – as SeS2 Hydrogen Peroxide in anhydrous glycerin (1.5%) Urea Peroxide in anhydrous glycerin (4-10%) Pharmaceutically relevant chemical forms: Carbamide Peroxide Topical Solution o Sulfide (-2 oxidation state)→ Hydrogen sulfide and soluble o More preferred for treatment of oral and ear infections sulfides react readily with finely divided sulfur to produce polysulfides, Sx-2 ZINC PEROXIDE AND SODIUM PERBORATE o Sulfite (+4 oxidation state) Former official compounds o Sulfate (+6 oxidation state OZONE, O3 SULFUR OINTMENT Powerful oxidizing agent→ Disinfectant, bleach (industrial) Prepared from precipitated sulfur, mineral oil and White Ointment 10% Sulfur SULFUR AND SULFUR COMPOUNDS SULFUR, S SULFURATED LIME Brimstone, Shulbari (Sanskrit: enemy of copper), Asupre Vleminckx’s Solution Several allotropes o At room temp.: α-Sulfur (rhombic sulfur) is stable SULFURATED POTASH Liver of Sulfur INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 18 Consist mainly of polysulfide, thuisulfate and sulfate CHROMIUM AND CHROMIUM COMPOUNDS Prepared by careful heating of a solution of potassium carbonate CHROMIUM, Cr and sublimed sulfur Glucose Tolerance Factor Used in the form of lotions, ointments, and aqueous solutions for Essential trace element treatment of psoriasis Deficiency symptoms are similar to that of DM Also has antiparasitic activity Forms o Hexavalent Chromium, Cr6+ WHITE LOTION Toxic Prepared from Sulfurated Potash and Zinc sulfate Dichromate→ strong oxidizing agent o Astringent and protective Primary standard – Sodium Thiosulfate VS Chromate →precipitant SELENIUM SULFIDE, SeS2 o Trivalent Chromium , Cr3+ SeS2 and SeS2 Lotion (Selsun Blue) 2.5% suspension used for the topical treatment of seborrheic CHROMIC CHLORIDE AND CHROMIC CHLORIDE INJECTION dermatitis CHROMIUM PICOLINATE o Hands should be washed off --- Se is toxic o Should not come in contact in eyes and mouth MOLYBDENUM AND MOLYBDENUM COMPOUNDS o Cadmium Sulfide, in the past, was also used for this purpose MOLYBDENUM, Mo Essential trace element SULFUR DIOXIDE, SO2 Cofactor for enzymes associated with flavin-dependent enzymes Acid anhydride of sulfurous acid Cofactor for Xanthine Oxidase Oxyacid: sulfurous acid Important for bacterial fixation of atmospheric oxygen Used pharmaceutically as antioxidant and preservative MOLYBDENUM OXIDE, MoO SODIUM METABISULFITE, Na2S2O5 with ferrous sulfate → hematinic Obtained when sodium bisulfite is crystallized on an atmosphere of sulfur dioxide URANIUM, U Forms bisulfite upon dissolving in water Should be used when sodium bisulfite is specified Radioactive element Antioxidant Discovered by Becquerel Never employed in medicine as such SODIUM THIOSULFATE, Na2S2O3 Used in atomic reactors and atomic bombs Prepared from sulfur reacing with sulfite ions Antidote for cyanide poisoning GROUP VIIA (17): HALOGENS Analytical reagent for determination of iodine Halogen = Sea-salt producer SODIUM SULFATE, Na2SO4 FLUORINE AND FLUORINE COMPOUNDS Saline cathartic FLUORINE, F2 Most electronegative element SELENIUM Strongest oxidizing agent SELENIUM, Se Selena→ moon SODIUM FLUORIDE, NaF Toxic → Prolonged contact with skin causes contact dermatitis Sodium Fluoride Tablets; Oral Solution Important trace element Sodium Fluoride and Phosphoric Acid Gel Absorbed very slowly on the skin Sodium Fluoride and Phosphoric Acid Topical Solution Promotes absorption of Vitamin E Also used in the treatment of osteoporosis Excess fluoride in adults: GROUP VIB (6) o Weakening of bones Chromium and Molybdenum→ Important trace elements o Adverse effects on the kidney o Low IQ INORGANIC PHARMACEUTICAL CHEMISTRY REVIEW 19 o Suppressive effect on thyroid, particularly when iodine is Bromine TS deficient Bromine Water→1% Bromine in water Excess fluoride in children→ dental fluorosis Bromine VS STANNOUS FLUORIDE, SnF2 Koppeschaar’s Solution easily air-oxidized 0.1 N Bromine VS Stannous Fluoride Gel Components SODIUM MONOFLUOROPHOSPHATE Br -→ internally acts as a sedative (depressant) Anticariogenic agent added in dentifrices Three Bromides Elixir CHLORINE AND CHLORINE COMPOUNDS IODINE AND IODINE COMPOUNDS CHLORINE, Cl2 IODINE, I2 Dephlogisticated muriatic acid Heaviest nonmetallic element Chlorine is used as a water disinfectant Easily undergoes sublimation, giving off violet vapor Cl- →principal extracellular cation Solid with metallic sheen Poisonous→ Antidote: Starch solution CHLOROFLUOROCARBONS I- Dichlorodifluoromethane, CCl2F2 o Expectorant o Freon o Antiseptic o Refrigerant; aerosol propellant o Essential trace element necessary for synthesis of T3 and T4 o Implicated in ozone layer depletion hormones o T3 – triiodothyronine – more active HYDROCHLORIC ACID, HCl o T4 – thyroxine – more numerous In diluted form→ treatment for gastric achlorrhydria o Toxicity: Iodism present in gastric juice o Deficiency state: Simple Goiter Pepsinogen is secreted by chief cells, which is activated by HCl Dangerous for pregnant women – cretinism secreted by parietal cells, to pepsin Prevention: iodized salt Diluted Hydrochloric Acid is official --- 10% w/v solution Iodine Preparations SODIUM HYPOCHLORITE, NaOCl Bleaching agent Disinfectant Sodium Hypochlorite Solution (Dakin’s Solution) o Effective germicide, viricide, and deodor