Organic Chemistry in Pharmacy

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Questions and Answers

Which type of molecule is characterized by having a primary active component that is a metal or inorganic element?

Peptides

Inorganic compounds (correct)

Organic compounds

Carbohydrates

Which of the following is NOT an example of an organic compound used as a drug?

Metal-based drugs (correct)

Anticoagulants from glycosides

Long chain fatty acids in nutritional supplements

Aldosterone hormone

Which property of peptides and proteins limits their potential routes of administration?

Stability in the gastrointestinal tract

Low potency

Large molecular size (correct)

High solubility in water

What is a major advantage of pegylated pharmaceuticals?

Extended half-life in circulation Signup and view all the answers

Which of the following therapeutic agents is based on monoclonal antibodies?

Immunotherapy drugs Signup and view all the answers

Given the generic name of a monoclonal antibody product, what can one identify?

The target and source of the product Signup and view all the answers

Which type of organic compounds includes steroid hormones?

Lipids Signup and view all the answers

Which of the following is classified as an inorganic drug category?

Ferrous sulfate Signup and view all the answers

Which type of organic compound can act as antiviral agents?

Nucleosides Signup and view all the answers

Which property associated with pegylated proteins enhances their pharmacokinetics?

Reduced immunogenicity Signup and view all the answers

What is the primary mechanism of action of Cisplatin in treating cancer?

Formation of interstrand and intrastrand crosslinking of DNA Signup and view all the answers

Which of the following fluoride salts is specifically mentioned as enhancing the strength of teeth?

Sodium fluoride Signup and view all the answers

What is the therapeutic use of bismuth subsalicylate?

Antiemetic and antidiarrheal Signup and view all the answers

Which of the following is a common property of silver salts used in medical applications?

Disrupts bacterial cell walls Signup and view all the answers

What therapeutic class do aminoglycosides, such as Tobramycin and Amikacin, belong to?

Antibacterial agents Signup and view all the answers

Which mechanism describes the action of Orlistat as an antiobesity agent?

Blocking the absorption of dietary fats Signup and view all the answers

What is the main use of Fludarabine phosphate?

Immunosuppression and treatment of B-cell CLL Signup and view all the answers

Which chemical class does Carboplatin belong to?

Metal therapeutics Signup and view all the answers

What effect do unnatural or modified amino acids have on peptide metabolism?

They decrease metabolism by peptidase/protease enzymes. Signup and view all the answers

What is the primary function of calcium halophosphate in tooth enamel?

Enhancing strength Signup and view all the answers

What distinguishes the therapeutic class of drugs like lithium carbonate?

Mood stabilization in bipolar disorder Signup and view all the answers

Which therapeutic agent was the first FDA-approved recombinant drug?

Humulin® Signup and view all the answers

Which statement accurately describes monoclonal antibodies (MAbs)?

They are derived from a single clone of antibody-producing cells. Signup and view all the answers

Which of the following is a characteristic of PEGylation?

It can improve the pharmacokinetics of modified proteins. Signup and view all the answers

What is the primary biological action of insulin?

To promote the synthesis of glycogen, proteins, and lipids. Signup and view all the answers

Which enzyme is NOT mentioned as a therapeutic agent for cardiovascular uses?

Asparaginase Signup and view all the answers

What is a potential benefit of using peptidomimetics in drug discovery?

They mimic the size, shape, and electronic distribution of peptides. Signup and view all the answers

Which therapeutic agent is specifically used for enzyme replacement therapy for ADA deficiency?

Pegademase bovine Signup and view all the answers

What is the primary reason for replacing Gly6 with modified amino acids in gonadotropin-releasing hormone?

To increase its half-life and potency. Signup and view all the answers

Which property is NOT associated with polyethylene glycol (PEG) in pharmaceuticals?

Increasing the frequency of dosing required. Signup and view all the answers

Study Notes

Inorganic Compounds

Platinum Compounds: Used for chemotherapy
- Cisplatin (Platinol®): First metal compound used for cancer treatment; Causes kidney damage
- Carboplatin (Paraplatin®): Less toxic than cisplatin
- Oxaliplatin (Eloxatin®): Also less toxic than cisplatin
Fluoride Salts: Used to strengthen tooth enamel
- Sodium fluoride (Prevident®, Ethedent®, Luride®): Helps form fluorapatite, which is a key component of enamel
- Stannous fluoride (Gel-Kam®, Flo-Gel®): Another form of fluoride used for dental health
Silver Salts: Used for preventing and treating infections, especially in burn cases
- Silver sulfadiazine (SSD®, Silvadene®): Disrupts bacterial cell walls
Bismuth Salts: Used as anti-emetics, anti-diarrheals, and antacids
- Bismuth subsalicylate (Pepto-Bismol®, Kaopectate®): Binds to toxins, promotes water and electrolyte absorption, and inhibits prostaglandin synthesis
Other Inorganic Compounds:
- Gold salts: eg. auranofin (Ridaura®) - Used for rheumatoid arthritis
- Iron salts: e.g. Ferrous sulfate (Feosol®) - Treats iron-deficiency anemia
- Lithium salts: e.g. Lithium carbonate (Eskalith®, Lithobid®) - Used for bipolar and manic disorders
- Zinc salts: e.g. Zinc acetate (Galvin®) - Used for lozenges, astringent, and Wilson's disease

Organic Compounds: Glycosides/Carbohydrates

Carbohydrates: Diverse biological functions
- Monosaccharide: One sugar unit
- Polysaccharide: Many sugar units
- Glycoside: A combination of a carbohydrate moiety (glycone) and a non-carbohydrate moiety (aglycone)
Aminoglycosides: Antibiotics that inhibit bacterial protein synthesis
- Tobramycin (Tobrex®, TOBI®)
- Amikacin (Amikin®)
Other Carbohydrate-Based Drugs:
- Alpha-glucosidase inhibitors (Antidiabetic agents): Acarbose, Miglitol
- Heparin & derivatives (Antithrombotic agents): Heparin, Dalteparin (Fragmin®), Enoxaparin (Lovenox®), Tinzaparin (Innohep®)
- Cardiac glycosides: Digoxin (Lanoxin®)
- Anthracycline glycosides (Anti-cancer agents): Doxorubicin (Adriamycin®, Rubrex®)

Organic Compounds: Nucleosides

Purine and Pyrimidine Analogues: Antivirals and anticancer agents
- Fludarabine phosphate (Fludara®): Used to treat B-cell chronic lymphocytic leukemia; inhibits ribonucleotide reductase

Organic Compounds: Lipids

Orlistat (Xenical®, alli®): Anti-obesity drug; inhibits lipase, blocking fat absorption
Omega-3 fatty acid esters (Lovaza®): Hypolipidemic agent

Peptides & Proteins

Delivery Issues:
- Oral administration: Poor absorption due to polarity and breakdown by peptidases and proteases in the gut
- Solutions: IV, Inhalation, IM, SC, modified amino acids, peptidomimetics, hydrogels
Drug Design Options:
- Modified amino acids: Increase resistance to proteolysis and increase half-life
- Peptidomimetics: Small organic molecules that mimic peptides
Hormones:
- Insulin (Humulin®): Produced by the pancreas; promotes glycogen, protein, and lipid synthesis, lowering blood glucose levels
Enzymes:
- Tissue plasminogen activators (t-Pa)/anticlotting enzymes (e.g. urokinase, streptokinase)
- Pegademase bovine (Adagen®): Enzyme replacement therapy for ADA deficiency
- Asparaginase (Elspar®): Depletes asparagine sources in cancer therapy
- Dornase alfa (Pulmozyme®): Used for cystic fibrosis via inhalation

Peptides & Proteins: PEGylation

Polyethylene glycol (PEG): Polymer of ethylene oxide commonly used in foods, cosmetics, and pharmaceuticals
PEGylation: Covalently attaching PEG to proteins; improves pharmacokinetic properties by decreasing metabolism, increasing half-life, and allowing for lower doses and frequencies

Peptides & Proteins: Monoclonal Antibodies (MAbs)

Antibodies (immunoglobulins): Secreted by activated B-lymphocytes
Monoclonal antibodies: Derived from a single clone of antibody-producing cells; highly specific for a single antigen/epitope
Nomenclature of MAbs:
- Source:
  - chimeric ("-xi-")
  - human ("-u-")
  - humanized ("-zu-")
  - murine ("-o-")
- Target:
  - bacterial ("ba(c)-")
  - cardiovascular ("ci(r)-")
  - immune ("li(m)-")
  - infectious lesions ("le(s)-")
  - tumors ("tu(m)-")
  - viruses ("vi(r)-")
Examples of Therapeutic MAbs:
- Trastuzumab (Herceptin®)
- Rituximab (Rituxan®)
- Ibritumomab tiuxetan (Zevalin®): Linked to a radionucleotide
- Efalizumab (Raptiva®)
- Bevacizumab (Avastin®)
- Infliximab (Remicade®)
- Abciximab (ReoPro®)
- Omalizumab (Xolair®)
- Daclizumab (Zenapax®)
- Palivizumab (Synagis®)
- Gemtuzumab ozogamicin (Mylotarg®): Linked to an antitumor antibiotic

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Description

Explore the use of various inorganic compounds in medical treatments. This quiz covers platinum compounds for chemotherapy, fluoride salts for dental health, silver salts for infection prevention, and bismuth salts for gastrointestinal issues. Test your knowledge on these essential compounds and their applications.