Inorganic Pharmaceutical Chemistry Review PDF

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 MgCO3CaCO3  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 3NaFAlF3 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)28H2O  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