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Inorganic Medicinal Chemistry


Pharmaceutical Chemistry 1

OVERVIEW
The Groupings of Elements
Elements are grouped according to their class exhibiting similar physical and chemical
properties.
The three (3) Systems of group numbering of elements:
 New IUPAC (The modern International Union of Pure and Applied Chemistry)- use of numbers
 CAS( Chemical Abstract Service)- used in U.S.
 Old IUPAC- use of Arabic/Roman Numerals

GROUP 0 (Group VIIIA or Group 18)


 Inert/Noble Gases
 All gases & non-reactive at low temperature; non-reactivity due to its closed outer orbitals
making its stable
 Members: Helium (He), Neon (Ne), Argon (Ar)
Krypton (Kr), Xenon (Xe), Radon (Rn)

1. Helium (He)
 Atomic weight:4.0026
 E- config: 2
 Date discovered & proponent: 1868, Pierre Janssen
 Origin: Greek “Helios” (sun) ; since it was detected in sun from its emission line in
the solar system
 Properties: non-flammable, inert, colorless, odorless
 Melting Point: -268.9 °C Boiling Point: -268.9 °C
 Source: natural gas
 Uses
- Component of artificial air (mixture of 80% He and 20% O2)
- Used in preparation of synthetic airs due to low density and low solubility in the
blood
- Used in cryogenic research, lasers, inflating balloon

2. Neon (Ne)
 Atomic weight: 20.1798
 E- config: 2-8
 Date discovered & proponent: William Ramsay & Morris Travers
 Origin: Greek “Neos” (new)
 Properties: colorless, odourless; glows orange when
electricity is passed through it
 Melting Point: 248.59 °C Boiling Point: -246.08 °C
 Source:
 Uses: NO PHARMACEUTICAL USE
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3. Argon (Ar)
 Atomic weight:39.948
 E- config:2-8-8
 Date discovered & proponent: 1894, John Rayleigh and William Ramsey
 Origin: Greek “Argos” (inactive due to inability to react with other elements)
 Properties: colorless, odourless, inert gas
 Melting Point:-189.3 °C Boiling Point: -185.86 °C
 Source: natural gas; 3rd most prevalent gas in the Earth’s atm
 Uses:
- Substitute of N2 as an inert atm for readily oxidizable pharmaceuticals
- Electric lights, gas shield in wielding

4. Krypton (Kr)
 Atomic weight: 83.798
 E- config: 2-8-18-8
 Date discovered & proponent: 1898, William Ramsey and Morris Travers
 Origin: Greek “Kryptos” (hidden due to difficulty in obtaining
air from it)
 Properties: colorless, odourless, inert gas
 Melting Point: -157.4 °C Boiling Point: -153.2 °C
 Source: Natural gas
 Uses:
- General anesthetic properties
- Fluorescent/incandescent bulbs
- Lasers emit bright light, orange-red color

5. Xenon (Xe)
 Atomic weight: 131.29
 E- config: 2-8-18-18-8
 Date discovered & proponent: 1898, William Ramsay & Morris Travers
 Origin: Greek “Xenon” (Stranger/foreigner)
 Properties: colorless, odourless, inert gas
 Melting Point: -111.8 °C Boiling Point: -108.1 °C
 Source: natural gas density: 5.9 g/L at 0°C
 Uses
- Stable fluorides in the form of diflouride, tetrafluoride, hexafluoride, crystalline Na
pexenate, perkryptate
- Diagnostic studies both inhalation and Iv injection
- General anesthetic properties
- Lighting devices in high speed photographic tubes
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6. Radon (Rn)
 Atomic weight: 222
 E- config: 2-8-18-32-18-8
 Date discovered & proponent: 1900, Friedrich Dorn
 Origin: Isotopes decay of Radium
 Properties: colorless odourless, radioactive gas
 Melting Point: -71°C Boiling Point: -62°C
 Source: radioactive decay of radium
 Uses
-Tx of certain cancer (Radiotherapy)

GROUP 1 A- ALKALI METALS


 found in nature combined with other elements
 low melting point, soft than other metals
 Has only 1 valence electrons; chemically stable cations, +1 oxidation state; forming salts
 Good reducing agents; most reactive of all metallic elements
 Free elements are NOT found in nature, since they are very active
 Form hydroxides (strongly basic); except LiOH; with H2, hydrides, halogens, halides
 Members: Lithium (Li), Sodium (Na), Potassium (K)
Rubidium(Rb), Cesium (Cs), Francium (Fr)

1. Lithium (Li)
 Atomic weight:6.941
 E- config: 2-1
 Date discovered & proponent:1817, Johan Arfwedson
 Origin: Latin “Lithos” (stone)
 Properties: silvery white, chemical reactive, metallic element; lightest weight of all
metals
 Melting Point:134.2°C Boiling Point: -108.1°C
 Source:
- Doesn’t occur in nature in free state, but ONLY in compounds( widely distributed)
- Obtained by electrolysis of a mixture of fused Li and KCl
 Specific gravity: 0.53
 Uses:
- Tx of hypomanic and manic states associated with bipolar disorders;
- Lithium carbonate Li2CO3 USP38/NF33
- Lithium citrate Li3C6H2O7 4H2O

2. Sodium (Na)
 Atomic weight: 22.9898
 E- config: 2-8-1
 Date discovered & proponent: 1807, Humphry Davy
 Origin: Latin “Natrium” (natural)
 Properties: highly-reactive, silvery white, extremely soft
 Melting Point:98°C Boiling Point: °C883
 Source:
-found in nature only in combined state; ocean, lakes
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Prepared commercially by electrolyte decomposition of NaCl


 Specific Gravity: 0.97
 Common used Na compounds
- NaCl (freezing salt, rock salt, table salt; electrolyte replenisher)
- Na2CO3 (sodium carbonate) 3 FORMS
A. Anhydrous Na2CO3 (soda ash)
B. Na2CO3 2H2O USP38/NF33 (trona)
C. Na2CO3 10H2O (soda crystals, sal soda, washing soda)

USES: topically used for dermatitis, mouthwash, vaginal douche; vet. used as
emergency emetic, antacids, and carbonating agent.
- NaHCO3 (sodium bicarbonate);baking soda-- metabolic acid
- Na2CO3 10H2O (sodium carbonate decahydrate); sal soda-- water softener
- NaOH( caustic soda/lye); hardener, increased lye can cause skin irritation
- Na2B4O7 10 H2O (Borax); astringent, nose and throat, water softener

3. Potassium (K)
 Atomic weight:39.0983
 E- config: 2-8-8-1
 Date discovered & proponent: 1807, Humphry Davy
 Origin: Latin “Kalium” (Alkali)
 Properties: extreme silvery white soft, metallic element
 Melting Point: 63°C Boiling Point: 760°C
 Source:
- found in nature in large qts.
- 8th in abundance of elements in Earth’s crust
- Major Cation of the intracellular fluid
- diuretic increase urine ouput
 Specific gravity: 0.53
 Commonly used K salts:
- K2CO3 (Potassium carbonate); potash--alkalizer,diuretic
- KNO3 USP38/NF33 (Potassium nitrate); saltpeter-- preservative in meats
- KNO2 (potassium nitrite)--vasolidating agent, applied precaution in Adverse
effects of hypotension
- KHC4H4O6 (cream of tartar)--sauce, dips, gravy

4. Rubidium (Rb)
 Atomic weight: 85.4678
 E- config:2-8-18-8-1
 Date discovered & proponent:1861, Robert Bunsen and Gustav Kirchoff
 Origin: Rubidus (deep red); prominent red line on its spectrum
 Properties: chemically reactive metallic element, silvery white, very soft
 Melting Point: 39°C Boiling Point: 688°C
 Source:
-widely distributed in Earth’s crust
- 16th abundant element in Erath’s crust
 Specific Gravity: 1.53
 Uses: NO PHARMACEUTICAL USE; used in making certain catalysts and in
photoelectric cells
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5. Cesium(Cs)
 Atomic weight: 132. 9054
 E- config:2-8-18-18-8-1
 Date discovered & proponent: 1860, Robert Bunsen and Gustav Kirchoff
 Origin: Latin ”Caesius” (sky blue)
 Properties: white soft, chem. Reactive metallic element
 Melting Point: 28°C Boiling Point: 671°C
 Source: 46 in abundancy
th

 Specific Gravity: 1.87


 Uses: NO PHARMACEUTICAL USE; used in making photoelectric cells

6. Francium (Fr)
 Atomic weight: 223
 E- config: 2-8-18-32-18-8-1
 Date discovered & proponent: 1939, Marguerite Perey
 Origin: France; where it was discovered
 Properties: unstable radioactive element
 Source: Uranium ore, made artificially from actinium and thorium
 Uses: NO PHARMACEUTICAL USE; heaviest of alkali metals, naturally radioactive,
extremely rare and most electropositive

7. Ammonia(NH3) and Ammonium (NH4)


 NH3 - HYPOTHETICAL akali metal, since it displays many of the properties of the
alkali metal ions.
 NH4 - salts therapeutically are carbonates & chlorides( ingredients in expectorant
preparations, bromides( CNS depressants)
 In aq. Solution, NH3 is a mild alkalizer
 Household NH3 - 10% NH3, known as 16 degrees Baume
 (NH4)2CO3 H2O - effective reflex stimulant and expectorant aid in coughing out
phlegm.

GROUP 1B (GROUP II)- THE COINAGE METALS


 employed in ornaments and coinage
 free in nature; easily recovered from their compounds by reduction
 NOT a very active metal; thus easily displaced by other metals
 Chemical reactivity decreases as atomic weight increases
 Weakly basic except for Ag2O
 Members: Copper (Cu), Silver (Ag), Gold(Au)

1. Copper (Cu)
 Atomic weight:63.546
 E- config: 2-8-18-1
 Date discovered & proponent: Prehistoric, unknown
 Origin: Greek “kuprus” (Cyprus)
 Properties: malleable, reddish, brown, metallic element
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 Melting Point: 1085°C Boiling Point: 2562°C


 Source:
- 25th most abundant element in crustal rocks
- Principal source: chalcopyrite and bornite, mixed sulfdes of Cu and Fe
- Essential trace element; small qty enhance the physiological utilization of Fe
- Occurs in respiratory pigment as hemocyanin, in many enzymes such as
cytochrome oxidase as cofactor and is widely distributed
 Specific Gravity: 8.95
 Official Cu compounds:
- C12H22CuO14 (copper gluconate)
- CuCl2 2H2O (copper chloride dehydrate
- CuSo4 5H2O (copper sulphate pentahydrate)--blue vitriol/blue stone
- 64Cu isotope-- mineral metabolism studies
- Copper (II) sulfate-- basis for Fehlings and Benedicts sol’n (classic tests for
aldehydes and ketones)
- Barfoed’s sol’n contains CuSo4
- Cu compounds are used in fungicides, insecticides, and algicide

2. Silver (Ag)
 Atomic weight: 107.8682
 E- config: 2-8-18-18-1
 Date discovered & proponent: prehistoric, unknown
 Origin: Anglo-Saxon “Seolfur”, Latin “Argentum and Luna” (Moon)
 Properties: malleable, white, lustrous metal, conducts heat and electricity better than
any other metal
 Melting Point: 962°C Boiling Point: 2162°C
 Source:
- 66th among elements in crustal rocks
- Most malleable and ductile of all metals except from Gold
 Specific Gravity: 10.5
 Commonly used silver preparations:
- Silver compounds have the ability to precipitate proteins and Cl2 in tissues
- AgNO3 (silver nitrate); lunar caustic USP38/NF33--germicidal agent, important
silver
- Toughened AgNO3 (silver nitrate)-- styptic agent which stops bleeding in small
cuts and wounds
- C10HgAgN4O2S (silver sulfadiazine)-- top germicidal wound; to prevent infection,
ecosystem prevent decomposition`

3. Gold (Au)
 Atomic weight:196.965
 E- config: 2-8-18-32-18-1
 Date discovered & proponent: Prehistoric, Unknown
 Origin: Latin “Aurum” (gold)
 Properties: soft, dense, corrosion-resistant bright yellow metallic
 Melting Point: 1064°C Boiling Point: 2856°C
 Source:
- Widely distributed, rare
- 75th abundance in Earth’s crust
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- Pure gold--malleable and ductile of all metals


- Gold--king of metals
- Gold compounds- tx of autoimmune disease (lupus erythematosus, rheumatoid
arthritis)
 Specific Gravity: 19.3
 Official used Gold preparations
- Official used Gold COMPOUNDS GIVEN Intramuscular for Rheumatoid arthritis
( aurothioglucose, gold Na thiomalate)
- Auranofin tablets-- tx of Rheumatoid arthritis (oral gold)
- 198Au -tx of malignancies, synthetic tx of cancer
- Incase of toxocity, “dimercaprol” is the tx of choice since it will form chelates with
heavy metals.

GROUP IIA (Group 2)- THE ALKALINE EARTH METALS


 Less reactive than alkali
 General reactive enough ut not found in free metals in nature
 Strictly metallic except amphoteric Be
 Strong reducing agents, not as strong as 1A
 Chemical activity increases as atomic radius increases
 Members: Beryllium (Be), Magnesium (Mg), Calcium (Ca)
Strontium )Sr), Barium (Ba), Radium (Ra)

1. Beryllium (Be)
 Atomic weight:9.0122
 E- config:2-2
 Date discovered & proponent: 1798, Louis-Nicholas Vauquelin
 Origin: Chief mineral beryl, Al Be silicate
 Properties: gray, white, metallic element, light, hard,
brittle, resist corrosion
 Melting Point: 1287°C Boiling Point: 2471°C
 Source:
- 51st in natural abundance in the Earth’s crust
- Components for many parts of supersonic aircrafts, x-ray tubes, computers,
lasers, televisions, oceanographic instruments, personal body armor.
- Extremely toxic when inhaled, injected, or absorbed
 Specific Gravity: 1.85
 NO THERPAEUTIC USE

2. Magnesium (Mg)
 Atomic weight:24.3051
 E- config: 2-8-2
 Date discovered & proponent: 1755, Joseph Black
 Origin: Greek “Magnesia” (Magnesium)
 Properties:relatively unreactive, light-silver white metallic element
 Melting Point: 649°C Boiling Point: 1090°C
 Source:
- 8th in natural abundance
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- Occur only in chemical combination with other elements (minerals such as


dolomite, magnesite, carnallite)
- Major physiologic ion in chlorophyll
- 2nd most abundant INTRACELLULAR cation in cell
- Natural Ca channel blocker--important in cardiovascular disease
- INSOLUBLE Mg compounds are used in gastric acid which neutralize the
stomach
 Specific Gravity: 1.74
 Mg preparations
- Mg(OH)2 (magnesium hydroxide)-- milk of magnesia/magnesia magma
- MgSO4 (magnesium sulphate)--epsom salt; antidote Ba poisoning
- Mg(C18H25O2)2 (magnesium stearate)
- MgO (magnesium oxide)--calcined magnesia
- Mg(C12H22CaO4)(magnesium gluconate)
- 27Mg - artificial radioactive isotope used in research involving photosynthesis

3. Calcium (Ca)
 Atomic weight: 40.078
 E- config: 2-8-82
 Date discovered & proponent: 1808, Humphry Davy
 Origin: Latin “Calx” (Lime)
 Properties: reactive silvery-white metallic element
 Melting Point: 842°C Boiling Point: 1484°C
 Source:
- 5th abundance in earth’s crust
- Not found uncombined in nature
- Malleable/ductile, Ca rapidly tarnishes to yellow on exposure air
- Indispensable, most abundant cation in the body
- Cation (hydroxyapatite)--major constituent of bones and teeth
 Specific Gravity: 1.55
 Official Ca compounds represented by the following:
- Antacids, electrolyte replenishers, Ca supplements
- Cation choice carry therapeutic active anions such as: C14H12CaN2O6 (Ca
aminosalicylate), C24H30CaN4O6 (Ca cyclobarbital)
- Artifical 45Ca isotope-- studies in mineral metabolism
 Other preparations:
- Cao (calcium oxide)- lime/quicklime-- various insecticides
- Ca(OH)2 (calcium hydroxide)-- slaked lime/hydrated lime; typical solution and
protective agent
- CaO+ CuSO4 -> Bordeaux mixture( algicide, fungicide)

4. Barium (Ba)
 Atomic weight:137.328
 E- config: 2-8-18-18-8-2
 Date discovered & proponent: 1808, Humphry Davy
 Origin: ”Barys” (heavy)
 Properties: soft, silvery, highly reactive toxic, metallic elemet
 Melting Point: 727°C Boiling Point: 1897°C
 Source:
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- 14th most common element


- 1/2000th of Earth’s crust
- All Ba compounds are soluble in water or in dilute acid are poisonous
 Specific Gravity: 1.66
BaSO4 (barium sulphate) USP38/NF33 -radiopaque agent used as contrast
medium in diagnostic procedures; ultrasound

GROUPIIB (GROUP12) THE VOLATILE METALS


 Have pseudo-inert gas due to presence of 10 additional electrons in the d orbital
 Metals form divalent ions except Hg(unique property of monovalent ion)
 Less active; form covalent compounds
 Basicity increases in group with increase in ionic radius with HgO(most basic), and ZnO
(soluble in alkali)
 Cd and Zn form complex ion easily, but Cd is stronger than Zn
 Hg don’t enter into complex formations
 Members: Zinc (Zn), Cadmium(Cd), Mercury(Hg)

1. Zinc (Zn)
 Atomic weight:65.409
 E- config: 2-8-18-12
 Date discovered & proponent: Prehistoric, unknown
 Origin: German “Zink” (tin)
 Properties: bluish-white crystalline metal, insoluble in hot/cold water, alcohol, acids,
alkalides, extremely brittle at ordinary T. but becomes
malleable between 120°C and 150 °C
 Melting Point: 420°C Boiling Point: 907°C
 Source:
- 24th in abundance in Earth’s crust
- Never occurs free in nature
- Central Trace element
- Present in All living organism, widely distributed in food
- Therapeutic applications; tx of various external surfaces of the body and in
conditions like wound healing and taste acuity
 Specific Gravity: 7.14
 Commonly used:
- Zn with Cr and Se-- beauty minerals; enhance skin, nails, hair appearance
- ZnCl2 (zinc chloride) USP38/NF33)--germicide
- Zn (CH3COO)2 (zinc acetate) USP38/NF33-- precipitate; germicide
- Strong ZnSO4 (zinc sulphate); zincosite; emetic
- Zinc compounds soluble in H20/gastric fluid
ZnO (Zinc oxide) zincite--poisonous, antidote for NaHCO3

2. Cadmium (Cd)
 Atomic weight: 112.41
 E- config: 2-8-18-18-2
 Date discovered & proponent: 1817, Friedrich Strohmeyer
 Origin: Latin “Cadmia” Calamine
 Properties: silvery white metallic element easily shaped
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 Melting Point: 321°C Boiling Point: 767°C


 Source:
- 65th in natural abundance in Earth’s crust
- Principal constituent of a mineral only in the rare greenockite
- Soluble Cd compounds-- astringents(shrinking, firming of tissues)
 Specific Gravity: 8.64
 Cd preparations:
- CdSO4 (cadmium sulphate)-- local astringent, eyes
- Cd(cadmium sulphide; greenockite-- tx of seaborrheic dermatitis( clinical term
for acute dandruff)

3. Mercury (Hg)
 Atomic weight: 200.59
 E- config: 2-8-18-32-18-2
 Date discovered & proponent: prehistoric, unknown
 Origin: Latin “Hydrargyrum” (Liquid silver, quicksilver)
 Properties: poisonous heavy, silvery white liquid metal( Liquid at room T)
 Melting Point: -39°C Boiling Point: 357°C
 Source:
- 67th in crustal rocks
- Occurs in pure form Or combined with silver in small amounts but is found
most often in the ORE cinnabar (HgO)
- True metal( only metal Liquid at room T)
- Hg and its compounds are extremely toxic
- Na formaldehyde sulfoxylate & egg albumin-- antidotes for Hg poisoining
- Ammoniated mercury- tx of impetigo, psoriasis, etc( skin conditions
 Specific Gravity: 13.55

GROUP IIIA (GRP 13 BORON FAMILY)


 +3 OXIDATION STATE
 Readily oxidize when heated in air, stable at ordinary T
 Oxides- readily reduced back to free metals
 Metals- react readily with S and halogens
 Hydroxides tend to show amphoteric properties with the exceptions of the top and bottom
elements of the group
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Electrolytes- are substances that contain ions which make it electrically conductive.
Electrolyte Solution- usually formed when salt is placed in a solvent (water) where individual
components dissociate.

Primary ions of electrolytes: Na+, K+, Ca+2, Mg+2, Cl-, HCO-3, PO-34
 Na (Sodium) - major extracellular cation; helps maintain body fluid
 K (Potassium) - major intracellular cation; muscle and neuron function
 Ca (Calcium) - stronger, denser bones, Vitamin D (absorption of Ca)
 Mg (Magnesium) - needed by enzymes that utilize ATP
 Electrolytes are important for the regulation of hydration in our body.

Causes of dehydration
 Prolonged Physical Activity and sweating
 Diarrhea
 Vomiting
 Lacrimation
 Excessive consumption of alcoholic beverages
 Diabetes mellitus

Electrolyte Solutions
1. Ringer’s injection (solution of 3 chlorides)
- electrolyte, and fluid replenisher

2. Lactated Ringer’s injection (Hartmann’s solution)


- electrolyte, and fluid replenisher

3. Ammonium Chloride USP (Sal ammoniac)


- electrolyte replenisher; used in Metabolic acidosis

4. Calcium carbonate (limestone, precipitated chalk, chalk)


- antacid, antidote to oxalic acid

5. Monopotassium phosphate (MKP, Potassium dihydrogen phosphate)


- buffer, one of components of Gatorade

6. Dipotassium phosphate (Dipotassium hydrogen orthophosphate)


- Buffer

7. Potassium phosphate (Tripotassium phosphate)


- Buffer

8. Sodium dihydrogen phosphate (Monobasic sodium phosphate)


- Buffer, leavening agent

9. Disodium hydrogen phosphate (Dibasic sodium phosphate)

10. Sodium phosphate (Tribasic sodium phosphate)

11. Sodium acetate (Sodium ethanoate)


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12. Sodium bicarbonate (Baking soda, cooking soda, bread soda)


- Antacid, leavening agent, tx of ASA overdose

13. Sodium chloride (Rock salt, dendrite salt, solar salt)


- Food seasoning

14. Sodium citrate- anticoagulant


15. Calcium lactate- antacid
16. Potassium acetate- hypokalemia
17. Potassium chloride- hypokalemia
18. Sodium lactate- antacid
19. Calcium chloride (Muriated lime)- hypocalcemia
20. Calcium citrate- anticoagulant
21. Calcium gluconate - hypocalcemia
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