Pharmacology of Drugs
Q1. What are the diuretics write any two drugs Acetazolamide, frusemide
→Drugs promoting urine output are known as diuretic drugs, which refer only to those agents that act directly on the kidneys.
→These drugs primarily increase the excretion of water and ions like sodium (Na+), chloride (Cl-, or bicarbonates HCO3-) from the body.
→Glomerular filtration, tubular reabsorption, and tubular secretion in kidneys determine the excretion of substances
It is also employed in the treatment of various disorders like diabetes insipidus, nephrotic syndrome, hypertension, nutritional oedema, oedema of pregnancy, and liver cirrhosis They also decrease the intracellular and cerebrospinal fluid pressure
Examples-
- Acetazolamide
- Furosemide
- Bumetanide
Acetazolamide
→Acetazolamide is the prototype carbonic anhydrase inhibitor.
→This type of diuretics inhibit carbonic anhydrase enzyme in the membrane and cytoplasm of epithelial cell.
Uses-
Acetazolamide is self-limiting in nature.
It produces adverse effects like acidosis and hypokalemia.
Thus, it is not used as a diuretic anymore, instead, it is currently being employed in the treatment of-
- Glaucoma
- Alkalinising Urine
- Acute Mountain Sickness
Stability and Storage Conditions-
- It can be stored up to 48 months
- It should not be stored above 25° C
- It should be stored in the original pack in order to protect from light and moisture.
Types of Formulations-
- Capsules
- Tablets
Popular Brand Names –
- Diamox
- Diamox Sequels
Q3. What are the Anti Tubercular Agent with example ?
→ Tuberculosis (TB) is an infective diseases most commonly affecting the lungs, and caused by Mycobacterium tuberculosis and Mycobacterium bovis.
→ Since TB is an it spreads via air in the form of small droplets Patients infected with pulmonary TB or laryngeal TB may the infection by sneezing, coughing, singing, or even while talking.
→ The infective droplets, once released into the air in there for a few hours due to their very small size.
→ Tuberculosis can be treated in a long-term, i.e.. 8 months to 3 years
→ Tuberculosis infection can be cured it proper treatment is given within time. Non tuberculosis mycobacterial infections are known as M. arium complex (MAC) as they are caused by M. alam, M. kansali, M. murinum, and M. scrofulaceum. These organisms are resistant the commonly used anti-tuberculosis drugs; thus along with the standard Jugh some newer agents like fluoroquinolones, amikacin clarithromycin, azithromycin, or rifabutin are used.
Isoniazid
→ Isoniazid (or isonicotinylhydrazine, INH) an organic compound used the first line drug for preventing and treating tuberculosis.
Uses-
It is used with other drugs in the treatment of active tuberculosis (TB) infection.
Stability Storage Conditions-
It should be stored in room temperature.
Types of Formulations –
- Tablet
- Solution
Popular Brand Names –
- Nydrazid
- Pms-Isoniazid
Q. Explain Antiviral Agent example Acyclovir.
Antiviral agents are used for treating viral infections.
Similar to antibiotics for bacteria, specific antivirals are effective against specific viruses.
Antiviral drugs, instead of destroying their target pathogen, inhibit their development.
→Since antiviral drugs are harmless to the host, they can be used to treat infections.
→They should be distinguished from viricides that are not medications but destroy virus particles outside the body.
→The available antivirals are mostly designed to help against HIV, herpes viruses (that mainly causes cold sores and genital herpes, however, can cause various other diseases), hepatitis B and C viruses (that cause liver cancer), and influenza A and B virus.
→Since the viruses replicate within the host cells, it is difficult to find targets for the drug that would interfere with the virus without harming the host cells.
→Due to this reason, designing safe and effective antiviral drugs is a difficult task.
Acyclovir
Acyclovir is a nucleotide analog antiviral that is used for treating infections like herpes simplex, herpes zoster, herpes labialis, and acute herpetic keratitis.
It is the first line drug to be used in the treatment of infections caused by these viruses.
Chemical Name- 2
Amino-1,9-dihydro-9-((2-hydroxyethoxy)methyl)-3H-purin-6-one
Uses-
- Acyclovir cream with hydrocortisone is used in recurrent herpes labialis, and shortening lesion healing time in 6 years and older patients
- Acyclovir ophthalmic ointment is used in acute herpetic keratitis
- Acyclovir oral tablets, capsules, and suspensions are used in herpes zoster, genital herpes, and chicken pox .
- Acyclovir buccal tablet is used in recurrent herpes labialis
Fungal infections
Enlist various fungal infections. Define and classify antifungal agents giving suitable examples.
Any disease caused by fungus is known as fungal infection, Fungi are heterotropic microorganism.
A fungal infection is also called mycosis, a skin disease caused by a fungus.
Mycotic infections of human are:
1. Dermatophytoses is a contagious superficial skin infections. The diseases produced are ringworm of foot, ring- worm of skin, hair, nails.
2. Candidiasis can affect the skin and mucus membrane.
3. Saprophytes invade skin and penetrate deep causing lymphatic, pulmonary and systemic mycoses.
Fungal infections are:
(i) Candidiasis: Caused by yeast candida. (ii) Blastomycosis: Caused by the fungus blastomyces. (iii) Ringworm: A common fungal infection. (iv) Vaginal candidiasis. (v) Fungal nail infections. (vi) Mucormycosis: Caused by mucormycetes. (vii) Onchomycosis. (viii) Histoplasmosis
Antifungal Agents
The drugs which are used in the treatment of fungal infections are called antifungal agents.
Classification of Antifungal Agents:
1. Antibiotics, e.g. amphotericin-ẞ, griseofulvin, nystatin.
2. Pyrimidine derivatives, e.g. 5-flucytosine.
3. Azoles/ Imidazoles e.g. clotrimazole , miconazole , ketoconazole.
4. Allylamines, e.g. terbinafine
5. Thiocarbanilic acid derivatives e.g. tolnaflate
6. Phenolic compounds e.g. salicylic acid
7. Diamidines e.g. stilbamidine.
8. Dyes e.g. Gention voilet, malachite green
9 Unsaturated fatty acids undecylenic acid
(b) Fluconazole (Diflucan)
• It is commonly known as “Diflucan”.
• It is used for both systemic and superficial fungal infections.
Chemical Name
α -(2, 4-Difluorophenyl)-α -(1H-1, 2, 4-triazol-1-ylmethyl)-1H-1, 2, 4-triazole-1-ethanol.
Properties- 1. It is a white crystalline powder. 2. It is slightly soluble in water. 3. It is soluble in organic solvents such as chloroform, propylene glycol.
Stability and Storage – It should be stored in a tightly closed container at a temperature Jess than 30°C.
Uses- 1. Fluconazole shows fungistatic activity. 2. It is used in the treatment of candidiasis. 3. Used to control oesophageal and oropharyngeal candidiasis. 4. An eye drop is useful in fungal keratitis. 5. Useful to treat vaginal candidiasis.
Pharmaceutical Formulations- 1. Fluconazole tablets IP 2. Fluconazole capsules IP 3. Fluconazole oral suspension IP 4. Fluconazole eye drops.
What are urinary tract anti-infective agents? Classify the urinary tract anti infective agents with examples.
The drugs which are used to treat or prevent infections of urinary tract are called urinary tract anti-infective agents.
Classification –
1. Quinolone derivatives -For example, norfloxacin, ciprofloxacin, moxifloxacin, ofloxacin lome floxacin.
2. Naphthyridine Derivatives – For example, nalidixic acid, enoxacin
3. Cinnoline derivatives- For example, cinoxacin.
4. Miscellaneous- For example, methenamine, nitrofurantioin, furazolidine.
Give the details of ‘ofloxacin’ as urinary tract anti- infective agent.
Ofloxacin
Ofloxacin is a synthetic fluonoquinolone antibiotic.
Chemical Name- 9-Fluoro-2,3-dihydro-3-methyl-104(4-methyl-1-piperazin-yl)-7- xo-7H-pyrido[1, 2, 3-de]-1,4,-benzoxazine-6-carboxylic acid.
Properties- 1. It occurs as a pale yellow or bright yellow, crystalline powder. 2. It is soluble in glacial acetic acid. 3. It is slightly soluble in water, dichloromethane and methanol.
Stability and Storage – It should be stored at room temperature and should be kept away from light and moisture.
Uses – 1. It is useful in the treatment of genitourinary, respiratory, gas trointestinal infections. 2. It is used in the treatment of bronchitis and pneumonia. 3. It is used for the treatment of pelvic inflammatory disease. 4. It is useful for the treatment of acute gonococcal urethritis.5. Used for the treatment of prostatitis caused by E.coli. 6. It is used for infections of skin and soft tissues.
Pharmaceutical Formulations- 1. Ofloxacin tablets IP 2. Ofloxacin oral suspension IP 3. Ofloxacin ophthalmic solution IP 4. Ofloxacin infusion IP
Brand Names- Oflox, Exocin, Zenflox, Zanocin, Tarivid.
Narcotic Analgesics (Opioid Analgesics)
Define and classify Narcotic Analgesics with examples.
Narcotic Analgesics-The drugs which produce narcosis along with analgesic effect are called narcotic analgesics. Classification-
1. Naturally occuring:- Morphine and its analogues e.g. morphine, codeine, hydromorphine, oxymorphine, diamorphine, ethylmorphine.
2. Synthetic drugs: (a) Morphanion analogues, e.g. levorphanol. (b) Benzomorphan analogues, e.g. pentazocin. (c) 4-phenylpiperidine analogues, e. g. pethidine. (d) Phenyl propylamine analogues, e.g. methadone, dextrapropoxyphone.
Uses of Narcotic Analgesics- 1. To relieve moderate to severe pain. 2. To suppress non-productive cough (antitussive) 3. To induce sleep in the presence of pain. 4. To control diarrhoea.
2. Give the details of “Morphine” as Narcotic Analgesic.
1. Morphine
It is a principle alkaloid obtained from opium. It belongs to phenanthrene class of alkaloids. It was the first narcotic analgesic discovered.
Properties- In occurs as white needle-like crystals It has bitter taste It is very slightly soluble in water It is levorotatory and is monophasic liquid. It is practically insoluble in ether and chloroform. The solution is sterilized by maintaining at 98-100°C for 30 minutes with bactericide or by filtration.
Stability and Storage- It should be stored in a well-tight closed container and protected from light.
Uses- As narcotic analgesic ,To treat diarrhoea, To suppress cough, As a pre-anaesthetic medication.,As a hypnotic when insomnia is due to pain.
Pharmaceutical Formulations- Morphine injection IP,Morphine and atropine injection.,Morphine and ammonium chloride mixtures., Morphine and ipecacaunha mixture,Morphine and kaolin mixture, Morphine hydrochloride solution,Morphine suppositories.
Brand Names- Zephrol, Duromorph, Astramorph, Morcontin
What are Narcotic Antagonist? Explain any three Narcotic Antagonists.
Narcotic Antagonists are the drugs which block the euphoric effects of opiates by attaching to opiate receptors. Narcotic antagonists are used as antidote to treat poisoning of narcotic analgesics. Examples: Naloxone, Nalorphine, Naltrexone.
(a) Nalorphine• It was the first clinical useful narcotic antagonist. It is a mixed opioid agonist-antagonist. • Nalorphine has less analgesic effect than morphine. It is also known as N-allylnormorphine.
Properties 1. It is a white crystalline powder. 2. It is odourless. 3. It is insoluble in chloroform and ether. 4. It is soluble in dilute alkali hydroxide solution. 5. It is sterilized by autoclaving or by filtration.
Stability and Storage It slowly darkens on prolonged exposure to light and air. Hence it is stored in tightly closed container at controlled room temperature and protected from light.
Uses- 1. As an antidote for morphine poisoning.2. Used to reverse the opioid overdose.
Pharmaceutical Formulations-Nalorphine injection.
Brand Names– Nalline, Lethidrone.
(b) Naloxone
It is a narcotic/opioid antagonist
Properties 1. It occurs as a white crystalline powder 2. It is freely soluble in water, dilute acids and strong alkali
Stability and Storage- It is stored in a tightly closed container protected from light
Uses- 1. As a narcotic/opioid antagonist. 2. To block or reverse the effects of opioid drugs. 3. Antidote for acute morphine poisoning.
Pharmaceutical Formulations-Naloxone hydrochloride injection.
Non-steroidal Anti-inflammatory Drugs (NSAIDs)
What are non-steroidal anti-inflammatory drugs (NSAIDs)? Classify NSAIDs with suitable examples. OR Classify analgesics and antipyretics giving examples.
These are the drugs which are used to relieve pain, reduce inflammation and also lower the elevated body temperature. The NSAIDs act by inhibition of the cyclo-oxygenase (COX) enzyme.Classification of NSAIDs-
1. Salicylates, e g. aspirin, sodium salicylate2. P-aminophenol derivatives, eg. paracetamol, phenacetin,3. Pyrazolone derivative, e.g. phenylbutazone, oxyphenbutazone metamizole.4. Indole acetic acid derivative, eg. indomethacin, sulindac5. Phenylacetic acid derivative, e g. diclofenac, aceclofenac.6. Propionic acid derivative, e g. ibuprofen, ketoprofen, fenoprofen.7. Oxicam derivatives, e.g. piroxicam, tenoxicam.8. Selective COX-2 inhibitors, eg. celecoxib, etoricoxib.9. Anthranillic acid derivative, e.g. mefenamic acid,
Write a note on Aspirin. Describe the salicylic acid derivative used as anti-inflammatory agent.
Aspirin Acid) [ASA]
Chemical Name-Ortho-acetoxy benzoic acid or 2-acetoxy benzoic acid
Properties: 1. It occurs a white crystalline powder.2. It is colourless. 3. It is odourless and has slightly bitter taste. 4. It is soluble in water, freely soluble in alcohol,
Stability and Storage- It should be stored in a well tightly closed container and protected from light and kept in a cool, dry place.
Uses- It is used as analgesic to relieve moderate pains like headache,toothache.It is used as antipyretic.It has an anti-inflammatory action and is used in the treatment of rheumatoid arthritis.It is used to treat gout.In high doses, it is used to reduce risk of myocardial infarction.
Brand Names-Disprin, Aspro, Anacin, Coldarin, Powerin, Codopyrin, Ecosprin, Zorprin, Asatavb, Durlaza.
Pharmaceutical Formulations- Aspirin tables BP, IP,Soluble aspirin tablet.,Aspirin and caffeine tablet,Dispersible aspirin and caffeine tablet
Stability and Storage Conditions- It should be stored at 59°F to 77°F (15°C to 25°C) and kept away from light.
Types of Formulations- Capsules, Tablets, Suspensions
Popular Brand Name- Zorivax
Isoniazid structure
Furosemide
→Furosemide is a benzole-sulfonamide-furan with fast onset and short duration of action. It is used for treating oedema and chronic renal insufficiency.
Uses-
It is used for the treatment of oedema related to congestive heart failure, liver cirrhiosis, and renal disease.
• It is also used either alone or with other antihypertensive agents for the management of hypertension.
Stability and Storage Conditions-
It should be kept at room temperature from 59°F (15°C) and 86° F (30°C)
This drug should be kept away from light.
This medication should not be stored in moist or damp areas like bathrooms.
Types of Formulations- Tablet, Solution
Popular Brand Names- Lasix, Diaqua-2, Lo-Aqua
Norfloxacin
Norfloxacin is a quinolone derivative.
Properties – 1. It is a white to pale yellow, crystalline powder. 2. It has melting point of 221°C. 3. Its molecular weight is 319.34.
Stability and Storage- It is stored in a tightly closed light resistant container.
Uses- 1. It is used as antibacterial agent. 2. It is used to treat urinary tract infections. 3. It is used to treat gynaecological infections. 4. It is used for the treatment of inflammation of prostate gland, gonorrhoea and bladder infection. 5. It is used to treat bacterial diarrhoea.
Pharmaceutical Formulations- 1. Norfloxacin tablets IP 2. Norfloxacin suspension. 3. Norfloxacin eye drops IP
Brand Names- Norflox, Uroflox, Actiflox, Alflox, Bacigyl, Norilet, Norbactin.
Ciprofloxacin
Ciprofloxacin is an antibiotic used to treat number of bacterial infections.
Properties- 1. It is a pale yellow, crystalline in nature.2. It is slightly hygroscopic powder. 3. It is slightly soluble in methanol. 4. It is very slightly soluble in ethanol but insoluble in acetone, ethyl acetate and methylene chloride. 5. It dissolves in acetic acid.
Stability and Storage- It should be stored in tight and light resistant containers at 2-25°C.
Uses- 1. It is used for the treatment of urinary tract infection, prostatis and acute diarrhoeal disease caused by E.coli, shigella, salmonella. 2. It is used for the treatment of gonococcal urethritis, chancroid. 3. Used to treat infections of skin, soft tissues, bones and joints, 4. Used for the treatment of respiratory tract infections. 5. Also used for controlling bronchitis and pneumonia.
Pharmaceutical Formulations- 1. Ciprofloxacin tablets IP. 2. Ciprofloxacin injection IP. 3. Ciprofloxacin eye drops IP.
Brand Names- Cilox, Cifran, Ciprobid, Ciprolet, Alcipro, Zoxan
Amphotericin-B
It is a polyene microlide antifungal agent.
Properties- It occurs as a yellow to orange powder. It is almost odourless and tasteless It is practically insoluble in water and in alcohol.
Stability and Storage – It is affected by light, air and even at room temperature. Hence, it is stored in tightly closed light-resistant containers at a temperature of 2° to 10°C.
Uses- It is effective in candidiasis, blastomycosis. In cryptococcal meningitis. For suppression of oral or intestinal candidiasis.
Pharmaceutical Formulations – Amphotericin-B cream. ,Amphotericin-B lotion, Amphotericin lozenges, Amphotericin-B ointment., Amphotericin-B injection. ,Amphotericin mixture.
Griseofulvin
Griseofulvin is obtained from the mold penicillium griseofulvin.
Properties- 1. It occurs as a white or pale cream coloured powder. 2. It is tasteless and odourless. 3. It is very slightly soluble in water.4. It is soluble in acetone and freely soluble in tetrachloroethane,
Stability and Storage- It is stored in tightly closed containers and kept away from oxidizing materials.
Uses 1. As an antifungal agent. 2. Used to treat dermatophytoses. 3. Used to treat ringworm infections. 4. Used to treat Tinca infections.
Pharmaceutical Formulations-
1. Griseofulvin tablets.
2. Griseofulvin capsules.
3. Griseofulvin oral suspension.
Brand Names
G-fulvin, Grisovin, Bifulvin, Grifulvin-V, Gris-PECT, Grisoral, Walavin.
Ketoconazole- It is a imidazole derivative.
Structure-
Chemical Name – 1-Acetyl-4-(4-[[2-(2,4-dichlorophenyl)-2(1H-imidazole-1-ylmeth- yl)-1,3-dioxolan-4-yl] methoxy] phenyl] piperazine.
Properties- 1. It is a white to off-white crystalline powder. 2. It is freely soluble in dichloromethane. 3. It is soluble in chloroform and in methanol. 4. It is sparingly soluble in ethanol. 5. It is practically insoluble in water and in ether.
Stability and Storage- It is stored in a well closed container protected from light and at con- trolled room temperature,
Uses- 1. It is a broad spectrum antifungal. 2. It is used to treat seborrheic dermatitis and fungal skin infections. 3. It is used orally to treat severe refractory cutaneous dermato- phytic infections. 4. Ketoconazole is used for the treatment of systemic fungal infections such as candidiasis, coccidioidomycosis, blastomycosis, histoplasmosis, chromomycosis, paracoccidioidomycosis.
Pharmaceutical Formulations: 1. Ketoconazole tablets IP 2. Ketoconazole lotion.3. Ketoconazole cream.4. Ketoconazole ointment. 5. Ketoconazole antidandruff shampoo.
Brand Names- Ketovate, Funginoc, Danruf, Nizrol, Funazole, Antanazol, Ketazole.
Write a note on Ibuprofen. OR Give details of propionic acid derivative used as anti-inflammatory agent.
Ibuprofen-It is a propionic acid derivative
Chemical Name -(RS)-2-(4-isobutyl phenyl) propionic acid.
Properties: It occurs as white crystals or white crystalline powder.It has a characteristic odour.It is very slightly soluble in water.It is soluble in aqueous solution of alkali
Storage- It is stored in a tightly closed container, penned from light and temperature
Uses-It is used to treat rheumatoid arthritis, osteoarthritis Dysmenorrhea. Neck pains,Pains in malignant disease, Dental pains, Muscle aches.
Pharmaceutical Formulations- Ibuprofen tablet IP, BP ,Ibuprofen and paracetamol tablet. IP, Ibuprofen cream I.P.
Brand Names- Brufen, Ibugesic plus, Alfam, Advil, Genpril, Ibular, Acifen, Em flam.
Describe the details of paracetamol.
Paracetamol (Acetaminophen)
It is a p-aminophenol derivative,
Chemical Name- Pacetamido phenol OR 4-acetamido phenol OR P-hydroxy acetan ilide
Properties It occurs as white crystals or white crystalline powder. It is odourless and has bitter taste. It is sparingly soluble in water, It is insoluble in ether and chloroform.
Stability and Storage -It should be stored in a well tightly closed container and protected from light
Uses- It is analgesic and antipyretic agent.It is used to relieve the pain from muscles and joints. of headache, and other pains arising
Brand Names-Crocin, Metacin, Calpol, Paramol, Albinol, Cipmol, Panadol damol
Pharmaceutical Formulations-Paracetamol tablet IP, BP, Paracetamol elixir, Paracetamol oral suspension .,Paracetamol syrup, Paediatric paracetamol elixir BP, Acetaminophen tablet USP, Acetaminophen elixir USP
(c) Naltrexone
It is a noroxymorphone derivative with competitive opioid antago nistic activity.
Properties 1. It is white crystalline compound. 2. It is very hygroscopic. 3. It is soluble in water.
Stability and Storage It is stored at room temperature away from light and moisture..
Uses 1. It is used for the management of alcoholism and addiction to opioid drugs. 2. It is used to treat cholestatic pruritus. 3. It is used in obesity. 4. It is used to treat opioid dependance. 5. It is used to treat severe pains.
Pharmaceutical Formulations 1. Naltrexone hydrochloride tablet. 2. Naltrexone tablet IP. 3. Naltrexone implantable pellet.
Brand Names- Nalores, Adepend, Antaxone, Celupan, Contrave, Embeda, Vivitrol. Naltima, Revia.
Describe the following analogues of morphine (i) Codeine
It is an alkaloid obtained from opium.
Properties It occurs as a white crystalline or colourless powder. It is odourless and has bitter taste. It is slightly soluble in water and freely soluble in alcohol. It is very soluble in dilute acids.
Stability and Storage It be stored in a well tightly closed container and protected from light.
Uses As narcotic analgesic. To suppress cough. To treat diarrhoea. As a sedative and hypnotics. Also used in combination with aspirin.
Pharmaceutical Formulations – Codeine phosphate BP, Codeine linctus BP. Codeine phosphate syrup IP Codeine phosphate tablet BP Codeine and aspirin tablet. Aspirin, phenacetin codeine tablet BP.
Brand Names- Codlin, Cosaka, Kefex., Corex, Codistar, Glycodin, Powerin
Diamorphine (Heroin)
• It is diacetyl morphine. • It is commonly known as heroin.
Properties 1. It appears white crystalline powder. 2. It is soluble in water and alcohol. 3. It is produced by acetylation of morphine.
Stability and Storage- It is stored in a tightly closed container at controlled room teropera ture and protected from light.
Uses 1. Used for the treatment of severe pain. 2. As a narcotic analgesic. 3. To treat severe pain associated with surgical procedures, myocardial infarction.
Pharmaceutical Formulations 1. Diamorphine hydrochloride tablet. 2. Diamorphine hydrochloride injection. 3. Diamorphine hydrochloride nasal spray. 4. Diamorphine hydrochloride powder for reconstination.
Brand Names
Diagesil, Udidyne, Ayendi, Diaphin.