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PHARMACEUTICAL CHEMISTRY

OF INORGANIC MEDICINALS

1
PERIODIC TABLE

Group 1A Alkali Metals


Group IB Coinage Metals
Group IIA Alkaline Earth Metals
Group IIB Zinc Group Metals
Group IIIA Boron Family
Group IIIB Scandium Subgroup
Group IV-A Carbon Family
Group IV-B Titanium Subgroup 2
PERIODIC TABLE
Group V-A Nitrogen Family
Group V-B Vanadium Subgroup
Group VIA Oxygen Family
Group VIB Chromium Subgroup
Group VIIA Halogen Family
Group VIIB Manganese Subgroup
Group VIII Iron Triad, Palladium Family,
Platinum Family
Group VIIIAInert gases 3
GROUP I-A (ALKALI METALS)

 Valence (+1)
 Most reactive element
 Do not occur free in nature
 Salts are soluble

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GROUP I-A (ALKALI METALS)

Cesium is the most active metal of the group


Francium exists only as an unstable radioactive
species.

Alkali metals form hydroxides that are strongly basic


except LiOH which is quite weak due to small size of
lithium atom and hence the somewhat covalent
character of the compound.
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GROUP I-A (ALKALI METALS)

The alkali metals react vigorously with water to form


hydrogen gas and the metallic hydroxides and for this,
they must be stored under the kerosene, coated with
paraffin or protected in some other ways.

MH + H2O  MOH + H2

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GROUP I-A (ALKALI METALS)

The alkali metals react vigorously with water to form


hydrogen gas and the metallic hydroxides and for this,
they must be stored under the kerosene, coated with
paraffin or protected in some other ways.

MH + H2O  MOH + H2

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GROUP I-A (ALKALI METALS)

2Na + H2  2 NaH
NaH+ H2O  NaOH + H2
2 Na+ F2 2 NaF
4Na + 2 H2O  4NaH + O2
Li2O + H2O  2 LiOH
4 Li + O2  2 Li2O
2 Na + O2  Na2O2
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K + O2  KO2
1. HYDROGEN “INFLAMMABLE AIR”
 Element with no therapeutic uses
 Lightest element
 Essential constituent of all acids
 Powerful reducing agent

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ISOTOPES

 Protium - most abundant


 Deuterium - heavy water
- manufacture of batteries
 Tritium - radioactive isotope

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H+ -monovalent cation
-hydronium ion

H- -hydrides anion
Uses:
 production of margarine
 balloons
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2. LITHIUM “EARTH STONE”
Flame test: Carmine red
• Lightest metal
Uses: Heat exchanger in air condition
Antidepressant
Diuretic
LiBr - antidepressant
Li2Co3 - drug of choice for mania(Lithase)

LiD - hydrogen bombs


12
LiOH - remove CO2 from the air
3. SODIUM “FROM NATURE”
Flame test: Golden yellow

 predominant cation in extracellular fluid


 produce osmotic effect in the body.

Pharmacology:
-fluid retention
-respiratory edema formation
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CH3COONa
 Diuretic

 Urinary and systemic alkalinizer

 Antacid

 Alkalinizing agent in Benedict’s solution 14


NaHCO3
• systemic / absorbable antacid
A/E: -rebound hyperacidity
-systemic alkalosis
-edema formation
• carbonating agent
• effervescence- CO2 release

CO2 -enhance palatability


-mask bitter taste 15
• NaH2PO4 (Fleet Enema)
• rectal administration

Uses:
• cathartic / laxative
• treatment of cystitis
• urinary acidifier
• pH buffer
16
METHENAMINE

 Prodrug

 Active in vivo

 Acidify by NaH2PO4

 Releases HCHO
17
NaHSO3
• Antioxidant (Reducing Agent)

Na2CO3
 Na2CO3- anhydrous “Soda Ash”
 Na2CO3 * H2O
 Na2CO3 * 2H2O-Trona
 Na2CO3 * 7H2O
 Na2CO3 * 10H2O -soda crystals
-washing soda
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-sal soda
NaCl

 “table salt”, “solar salt”, “rock salt”

 electrolyte replenisher (NSS, Ringer’s)

 adjust tonicity

 preservative, condiment
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Na3C6H5O3
 Alkalinizer, buffer
 Diuretic
 Expectorant
 Shortens coagulation of blood
 Denige’s test- specific test for citrate

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NaF - anti cariogenic
- 2% (4 application)

NaOH -“caustic soda”, “sosa”, “lye”


- saponifying agent (hard soap)

Na hypophosphite
21

-reducing agent
NaOCl
 “Dakin’s solution”
 Bleaching agent
 Disinfectant
 Oxidizing agent

Diluted NaOCl
• (modified dakin’s solution)
• Antiseptic
22

• Irrigating solution (wash)


NaI
• Expectorant
 Solubilizer of I2

NaC3H6O3
 in the body
 Converted to HCO3
 Antacid
 Alkalinizer 23
NaNO2
• Antidote for CN¯ poisoning
 Vasodilator

CN¯-acts on cytochrome oxidase with high affinity


to methemoglobin.

Na2S2O3 – converts CN¯ methemoglobin to SCN¯ 24


NaNO3
• “chile salt peter”
 preservative

Na Monohydrogen PO4
 Na2HPO4

Na2SO4
• “glauber’s salt”
25
 cathartic
Na2 C 4 H 4 O 6
• 1° standard of Karl Fischer Titration

NaSCN
• hypotensive agent

Na2S2O3
• “photographer’s hypo”
• Antidote for CN¯ poisoning
• Standard volumetric solution for iodometry 26
3. POTASSIUM (K⁺
“KALIUM”)
Flame Test: violet
- predominant intracellullar cation
Pharmacology:
• Diuretic
• muscle contraction

Hypokalemia
27

• can cause muscular paralysis lead to death


KCH3COO¯
catalyst, deicer, extinguishing agent, preservative, alkalinizer

KHCO3
alkalinizer, fungicide, extinguishing agent, buffering agent

KHC4H4O6
• “cream of tartar”, “creamor”
Use: laxative

KBr
• antidepressant
K2CO3
28

• manufacture of glass, resp. equipment


KClO3
• component of toothpaste, gargles mouth washes due to
its oxidizing cleaning, deodorant action.

KCl
• Hyperkalemia

ANTIDOTE: Insulin, NaHCO3

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K Citrate
• Expectorant, diaphoretic

KOH
• “caustic potash”, “lye potash”
• Saponifying agent

KI
• Expectorant
• Solubilizer in I2

KNO3
• “salitre”, “salt peter”, “salt prunelle”
30

• Preservative, gun powder


KMnO4
• “mineral chameleon”
• Oxidizing agent, fungicide
• Volumetric solution in permanganometry

K2HPO4- catharthic
KNaC4H4O6
• “rochelle’s salt”, “siegnette salt”

• sequestering agent, cathartic, Fehling’s sol’n ingredient

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KSCN- hypotensive agent


SULFURATED POTASH “LIVER
OF SULFUR”
• mixture of K polysulfides and K2S2O3
• use in preparation of white lotion
• treatment of parasitic infection
• Treatment of acne & psoriasis

White Lotion
• with ZnSO4 and ZnS 32
AMMONIUM
• NH4⁺
• hypothetical alkali metal
Pharmacology:
• Diuretics
• Buffer
• Expectorant
• Anticariogenic

Haber’s Process- method of preparation


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Household NH3, NH3 H2O, dil. NH3 sol’n (10%)
(NH4)2CO3

• “Sal Volatile”
• “Salt of Hartshorn”
• Preparation of aromatic NH3 spirit
• Respiratory stimulant
• Baker’s ammonia

Aromatic NH3- “Spirit of Hartshorn”


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NH4CL
• “Muriate of Hartshorn”
• Urinary acidifier

Ammoniated Mercury
• “White Precipitate”
• Topical anti-infective

NH4I
• photographic chemical

NH4CH3OO
35

• spirit of mindererus
4. CESIUM
• catalyst in polymerization of resin forming materials.

5. Rubidium
• used in the manufacture of vacuum tubes and cathode ray
tubes (CRTs), and is used in some atomic clocks.

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FRANCIUM

• “eka-caesium” “actinium K”
• 2nd least electronegative element
• Highly radioactive (At, Ra, Rn)
• Due to its instability and rarity, there are no
commercial applications for francium.

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GROUP I-B (COINAGE METAL)
• Employed for ornamental and coinage purposes

• Free metal state

• Readily act as central unit of complexes / chelates.

38
1. COPPER
Cu⁺ (brown)
Copper
Cu⁺2 (blue)
• only reddish color metal
• 3rd malleable
• 3rd best conductor of electricity
• use in H2O purification
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Alloys - solution of 2 or more metals
Brass – Cu + Zn
Bronze – Cu + Sn
• occurs in respiratory pigment:
• hemocyanin
• cytochrome oxidase

Pharmacology:
• protein precipitant (astringent, antiseptic) 40

• enhance absorption / utilization of iron


WILSON’S DISEASE
• Copper poisoning
Antidote: Penicillamine
CuSO4
• “blue stone”, “blue vitriol”
• use in preparation of Benedict’s, Fehling’s, Barfoed’s (for
reducing sugar)
• Cu ⁺2- Cu2O (+) brick red precipitate
• local emetic
• combine with iron for hematinic property
• Antidote for phosphorus poisoning 41

• algicide and fungicide in swimming pool


Phosphorus Poisoning
• luminous vomiting
• garlic odor

CuSO4 + CaO
• “Bordeaux Mixture”

Copper Aceto Arsenate


• “Paris green” (insecticide)

Cuprous Citrate 42

• astringent
2. SILVER
• “Argentum”
• “shining” or “bright”
• only metal with oligodynamic action
• protein precipitant
• 2nd most malleable metal
• 2nd best conductor of electricity
43
Toxicity:
Argyria- darkening of skin

Antidote: NaCl

Ag + NaCl AgCl
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AgNO3
• “Lapiz Infernularis”
• “Lunar Caustic”
• “Indelible Ink”
• “Caustic Pencil”

Pharmacology:
• treatment of warts
• antiseptic for eye of baby with gonorrhoeal mother
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AMMONIACAL SILVER
NITRATE
• “Howe’s Solution”
• Dental protective and desensitizing agent

Tollen’s Reagent
• (+) silver mirror
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SILVER IODIDE
• Germicide
• Silver Proteinates
• Mild Ag Protein - “Argyrol”
19-25% antiseptic
• Strong Ag protein - “Protargol”
- 7.5-8.5% germicide for
ears & throat
• Colloidal Ag protein - “Collargol”
47

-18-22% general germicide


3. GOLD
• “Shining dawn”
• King of all metals
• Most malleable & ductile
• Best conductor of electricity
• Gold Preparations used in treatment of arthritis:

• Aurothioglucose
• Gold Sodium Thiomaleate
• Auronofin 48
GOLD
AQUA REGIA
• Composed of 3HCl : 1 HNO3
• dissolves gold

49
GROUP II-A (ALKALINE EARTH
METALS)

1.BERRYLIUM
• Extremely toxic metal

• Use in fluorescent lightning industry

• Can cause lung carcinoma, chronic granuloma

50
2. MAGNESIUM
• Lightest of all structurally important metals

SOURCES:
• Silicates -talc, asbestos

• Carbonates –magnesite, dolomite

• Sulfates- Keiserite 51
MAGNESIUM
• 2nd most abundant intracellular cation

• Metal present in chlorophyll

• Grignard’s Reagent (RMgX)

52
Pharmacology:
• Laxative
• Depressant
• Natural Ca++ channel blocker

Ca Gluconate
• Antidote for Magnesium poisoning
53
MgSO4
• “Epsom salt”

USES:
• Laxative
• Antiphlogistic
• Eclampsia
• Anti-convulsant
• Antidote for Ba2+ , Barbiturate poisoning 54
MgCO3
• “Magnesia”

USES:
• Antacid
• Carbonating agent
• Laxative
55
Mg(OH)2
• “Milk of Magnesia”
• “Magnesia Magma”

USES:
• Antacid
• Laxative
56
MgO
• “Calcined Magnesia”
• Component of universal antidote

Mg Trisilicate
Advantage:
• Protectant
Use:
57

• Protective coating
Hydrated Mg silicate
• “Talc”
• “Soap Stone”
• “French Chalk”
• softest mineral known
• filtering aid
• clarifying agent
• dusting powder to gloves 58
Mg Citrate
• “Lemonada Purgante”
USE:
• cathartic

59
3. CALCIUM
• 2nd most abundant extracellular
Flame Test: brick red
SOURCES: -dolomite -fluoride
-gypsum -phosphate rock
-apatite
• Major component of bones & teeth
• Muscles contraction
• Blood coagulation
60

• Neurotransmission
CALCIUM
Vitamin D
• Sunshine vitamin
• Absorption of calcium

DEFICIENCY:
• Osteomalacia
• Rickets 61
CaBr2
used for drilling fluid, food preservative, photography, fire retardant

CaCO3
• precipitated chalk
• prepared chalk
• Ingredients for dentrifice & toothpaste

CaCl2
• muriate of lime
62
Calcium Hydroxide
• “Slaked Lime”
• “Milk of Lime”

Calcium Gluconate
• Antidote in Magnesium Poisoning
• Ca++ supplement

Calcium Lactate
63

• Ca++ supplement
CaO
• “Quick Lime”
• Calx
• preparations of various insecticides

CaHPO4
• Ca ++ supplement

Ca3(PO4)
• “Bone ash” 64

• Antacid
CaOCl
• Chlorinated lime
• Chloride of lime
• Bleaching agent
• Disinfectant

CaSO4
• ½H2O
• “Plaster of Paris” “Gypsum “
• CaSO4. 2 H2O
• Terra alba
65

USE: preparations of dental impressions and surgical cast


4. STRONTIUM

• Flame Test: Crimson Red

• Use in production of red pyrotechnics

66
SrCl2
• Temperature desensitizing agent

• Active ingredients in Sensodyne@

67
5. BARIUM
• “Heavy”
• Flame Test: yellow green
• Use in green Pyrotechnics

Toxicity:
• BARITOSIS

Antidote:MgSo4 68
BaSO4
“Barium Meal” “Sulfato de Bario”
“Esophotrast”
• Radiopaque medium for GIT imaging

Ba(OH)2
• CO2 absorber 69
6. RADIUM
• Discovered by Marie Curie

• Cancer chemotherapy

• Diagnostic purposes

• Becquerel (SI unit)


70
GROUP II-B
(VOLATILE METALS OR ZN FAMILY)

•  Zinc

• Cadmium

• Mercury
71
1. ZINC
• Rinman’s Green Test
• Container for batteries & dry cell
• Coating for galvanized iron
• Metal in insulin
• Constituent of carbonic anhydrase enzyme

Pharmacology:
-astringent, antiseptic, protectant, antiperspirant
72
Deficiency:
• Anemia and hypogonadism in male
• Stunted growth

Parakeratosis
• Thickened inflammed skin

Antidote: NaHCO3 73
ZnCl2
• Burnet’s disinfecting fluid, Butter of Zinc
• Escharrotic
• Antiseptic in mouthwashes
• Dentin desensitizer
• Use as corrosive
74
ZnO
• “Zinc White”
• Flowers of Zinc
• Lassar’s paste
• Component of Calamine lotion
• Antiseptic, protective, astringent
75
ZnSO4
• “White Vitriol”
• Emetic (internal)
• Astringent
• Pharmaceutical necessity for white lotion

ZnS
• “White Sulfide”
• Component white lotion 76
Hydrated Zn Silicate
• “Natural Calamine”
• ZnSiO4.1 H20
• protectant

Caladryl
• ZnO+Fe2O3 

Zn Eugenol Cement
• Dental protectant 77
ZINC
LITHOPONE
• A mixture containing 30% ZnS and 70%
BaS.

78
2. CADMIUM
• Manufacture of stink bomb
• Astringent
• Cadmium induces the synthesis of metallothionein, a protein
with a high binding affinity for cadmium.

• Metallothionein acts to protect certain


organs such as testes.
• Itai-itai poisoning
ANTIDOTE: BAL 79
CdCl2
• Anti-infective
• Emetic
• Treatment of tinea infection

CdS
• “Yellow Sulfide”
• Component of Capsebon
• Antiseborrheic

CdSO4
• Ophtalmic antiseptic 80
3. MERCURY
• “Quick Silver”, Liquid Silver, Liquid Metal, Noble Metal
• “Messenger of Gods”
SOURCE:
Cinnabar/Aethrop’s mineral(HgS)
• Hg+1
• Hg+2-toxic

Use: Manufacture of Thermometer


81
MERCURY
AMALGAM
• alloys of Hg
• Pasta
Pharmacology: -diuretic -antiseptic
-antisyphilitic -cathartic
-parasitacidal & fungicidal
-dental permanent cement
• Poisoning: Minamata disease
• Antidote: EDTA
Na formaldehyde sulfoxynate (Hydrargism) 82

Albumin – emergency antidote


Hg2Cl2
• Calomel
• Cathartic
• Local antiseptic

HgCl2
• Corrosive sublimate
• Disinfectant
83
HgI
• Anti-syphilis

HgI2
• Stimulant for indolent ulcers

K2HgI4
• Mayer’s reagent
• Test for alkaloids
84
Ammoniated Mercury
• “White Precipitate”
• Topical anti-infective

HgO
• “Yellow Precipitate”
• Ophthalmic antibacterial 85
GROUP III-A (BORON FAMILY)
1. Boron
• Non-metal
• Component of glass
• Flame Test: green bordered flame

• SOURCES:
Tincal – Na3BO3
H3BO3 86
• Hardness of Crytalline Boron
• Valuable substitute for diamond in glass
cutting and gem polishing.

87
BORATES
• Turmeric paper

• Use in vulcanizing rubber

88
H3BO3
• “Boric acid”, “boracic acid”, “sal sedativum”
• Toxic by ingestion
• Absorbed in broken skin
• Buffer in ophthalmic preparation
• Tonicity adjusting agent
• E-VALUE=0.52
• Antiseptic
• Eyewash: 2.45% - 2.5% 89

• Boroglyceringlyceride – suppository base


Na2B4O7
• Borax
• Sodium tetraborate
• Dobell’s Solution
• Eye wash
• Component of cold cream and in the preparation of
sodium borate preparation.

90
2. ALUMINUM
• Most abundant metal
• 3rd abundant element in earth’s crust
• Thenard’s blue test
• Abrasive in industries
SOURCES:
• Cryolite
-(Na3AlF6, sodium hexafluoroaluminate)
• Chief Source: Bauxite ore 91
Pharmaceutical Uses of Aluminum:
 Deodorant
 Protectant
• Antiseptic
• Antiperspirant

92
Aluminum Foil
• Treatment of Burns

Adverse Effects:
 Constipation

Toxicity: 93

• Shavers disease
AlCl3
• astringent, antiseptic, component of deodorant

Al(OH)3
• Amphojel
• Cremalin gel
Adverse Events:
• Constipation
• PO4 deficiency
94
AlPO4
• “Phosphagel”
• Antacid
• Astringent

Al2(CO3)3
• Treatment of phosphatic calculi

95
Alum
• Al K(SO4)2.12H2O
• Deodorant

Al2O3
• Alumina
• Treatment of silicosis
96
Aluminum Acetate
• Al(CH3COO-)3
• Burrow’s solution, Domeboro’s soln
• Astringent

• Dihydroxyaluminum amino acetate


• Gastric antacid
• Magma and tablet
97
Al Silicates
• KAOLIN
-”native hydrated aluminum silicate”, “china clay”
-adsorbent & demulcent in diarrhea

• BENTONITE
-“native hydrated colloidal Al silicates
-mineral soap, soap clay
- suspending agent

• PUMICE
-”Na, K, Al silicates”
-volcanic origin
98

-dental abrasive, dentrifice


3. Gallium
• Substitute for Hg in manufacture of arc lamps.
• Treatment of cancer related hypercalcemia.

4. Thallium
• “Thalos”
• Green twig
• 2nd most toxic metal 99
GROUP III-B (SCANDIUM
SUBGROUP)
Scandium
Yttrium
Lanthanum
Lanthanides (atomic # 58-71)
Actinium
Actinides (atomic # 90-103)
100

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