Friday, July 25, 2008

analgesics

© Okereke P. 2007

+2348055318800

Published by Noble publishers (A div. of Noble resources Ltd.)

1st print 2003

2nd print 2007 with amendments

Second edition 2007

COPYRIGHT RESERVED

No part of this publication may be reproduced in any for, electronic, mechanical, photocopying, recording or otherwise without the written permission of the publishers.

ISBN 978-2994-70-7

Second print by

Re-opec (Nig) Ltd.

9, st. John street/Modebe Avenue

Onitsha

+2348055523019

Preface

There are many drugs in the market today but only few of them are essential. The essential drugs according to World Health Organization are those drugs that satisfy the health care need of the majority of the population. One of the essential elements of Primary Health Care is “provision of essential drugs” and drugs makes health care credible because they have the ability to cure and prevent diseases, relieve symptoms and control any abnormal condition of the body. So many of drugs are in circulation in the drug market today and as such, problem of selecting the appropriate drug for a particular illness has been a hindrance to health practitioners. The introduction of essential drugs by the World Health Organization has helped to alleviate this problem.

Therefore the purpose of this book is not to make suggestions, create additional or separate list of essential drugs apart from the already existing list of the essential drugs of World Health Organization/Nigeria. Rather it is aimed at giving essential information (indication, mode of action, side effects, contraindications, route of administration, dosage schedule, safety precautions and examples of popular brand products that contains the required generic preparations) on rational used of drugs.

Finally all doses recommended in this book are for adults except where otherwise stated.

---Author

CONTENTS

Text Box: CONTENTS1. Anaesthetics and preoperative drugs 7

2. Analgesics,Antipyretics and NSAIDs 10

Narcotic 10

Non narcotic 12

NSAIDs 13

3. Anti allergics and antianaphylaxis 18

Antihistamines 18

Antianaphylactic 21

4. Antidotes 24

Specific 24

Nonspecific 24

5. anticonvulsants/antiepileptic 28

6. Antiinfective 32

Antihelmintics 32

Antifilariais 34

Antischistosomal 36

Antibacterial 37

Anti TBL 60

Antifungal 63

Antiviral 67

Antigiardiasis and antiamoebic 71

Anti malaria 72

7. Hormones and endocrine drugs 80

Corticosteroids 80

Androgen 82

Oestrogen 83

Progestogens 84

Contraceptives 85

Pituitary drugs 87

Anti diabetics 90

8. Antiparkinsonism 93

9. Drug affecting the blood 94

Antianaemia 94

Plasma substitute 97

Anti coagulants 97

10. Cardiovascular drugs 100

Anti anginal 100

Anti arrhythmic 102

Anti hypertensive 103

Cardiac glycosides 108

11. Dermatological drug 109

Antiinfective 109

Anti-inflammatory and antipruritic 110

Fungicides 112

Scabicides and pediculicides 114

12. Ophthalmic drugs 116

Antiifective 116

Anti-inflammatory/antiallergic 118

13. Antiseptic and Disinfectants 120

14. Diuretics 123

15. Gastrointestinal drugs 126

Antacids/antiulcer drugs 126

Anti emetic 129

Antispasmodic/smooth muscle relaxant 133

Purgative 134

Anti diarrhea 137

Antihaemorrhoid 138

16. Immunological 140

Sera and immunoglobulins 140

Vaccine 142

17. muscle relaxant 145

Myasthenia gravis 146

18. Oxytocics 148

19. Psychotherapeutic drugs 150

Hypnotics and sedatives 150

Anti psychotic 153

20. Respiratory drugs 158

Anti asthmatic 158

Antitussive and expectorants 159

21. Vitamins and minerals 162

22. Electrolytes 169

23. Ear, Nose and Throat drugs 172

Antiifective 172

Anti-inflammatory 173

Nose 174

Mouth and throat 176



2. ANALGESICS, ANTIPYRETICS AND NSAIDS

Analgesics (Painkillers) are a class of drugs used to relieve pain. The pain relief induced by analgesics occurs either by blocking pain signals going to the brain or by interfering with the brain's interpretation of the signals, without producing anaesthesia or loss of consciousness. There are basically two kinds of analgesics: non-narcotics and narcotics.
Non-narcotics - Non narcotic analgesics are effective in relieving mild to moderate pains and are further classified into two: i. anti pyretic and ii. Non steroidal anti-inflammatory agents

Narcotics - Narcotic analgesic alleviates severe pains and is capable of producing sedation even at moderate doses.

It is not fully understood how painkillers work. Damaged or inflamed body tissues produce various chemicals which send signals through the nervous system to the brain. The brain produces the sensation of pain. Different painkillers act at different points in this process. For example, NSAIDS may act at the point of injury, whereas others act on the nerves or brain.

I. Narcotic analgesics

DIHYDROCODEINE

30 mg (tartrate)/tab; 500 mg/ml amp.

A less potent narcotic analgesic used to relieve moderately severe pain; normal dose is 30 to 60 mg every six hours is for adults. This medication may cause dependence, especially if it has been used regularly for an extended time or if it has been used in high doses. In such cases, withdrawal reactions (e.g., runny nose, watery eyes, and restlessness) may occur if you suddenly stop this drug. To prevent withdrawal reactions when stopping extended, regular treatment with this drug, gradually reduce the dosage

Synonym: DF 118

MORPHINE

10 mg, 15 mg (sulphate or hydrochloride)/ amp, and 10mg (sulphate)/tab.

Is a powerful opiate derivative and is mostly suitable for severe continuous pain of visceral or soft tissue origin especially where other narcotic analgesic have failed. It is better to start therapy with oral dose of 2.5 to 5 mg every four hours. Dose may be titrated by 50 to 100% to control pain for full 24 hours. Morphine causes respiratory depression but does not alter blood pressure just like other opiate analgesic. Constipation with morphine is severe therefore it may be administered together with laxatives and antiemetic if vomiting occur. Contraindications include respiratory depression, obstructive airway disease, 24 hours pre and post operation, pregnancy, head injury, lactation and coma. S/E: tolerance, dependence, constipation, nausea, vomiting, drowsiness, urticaria. Morphine may be given in a dose of 10 to 20 mg either by s.c, i.m, or i.v injection.

PETHIDINE

50 mg/tab; 50 mg/ml (HCl)

Pethidine hydrochloride is an effective analgesic that can be used in place of morphine for the relieve of most severe types of pain. The analgesic action of pethidine hydrochloride is sometimes accompanied by euphoria; its duration of action may last for 2-5 hours. The dose varies with the purpose, age and route of administration. For relieve of pain in most medical and surgical condition, a dose of 100 mg i.m, orally or slow i.v injection. In severe pain, a dose of 150 mg may be required; up to 50 mg may be given as a single slow intravenous dose. Pethidine reduces the severity of labour pain, but does not alter contraction. A dose of 100 mg intramuscular is used for this purpose. S/P: Pethidine may cause respiratory depression

PETHILORFAN

Inj., pethidine 50mg (HCl) plus Levallorphan

0.625mg (tatrate) in 1 or 2ml ampoule

A nice combination of pethidine hydrochloride and levallorphan tartrate. The actions of pethidine are as enumerated above. Levallorphan prevents respiratory depression due to pethidine and other narcotic analgesic. Therefore pethilorfan exhibit all the analgesic actions of pethidine but does not cause respiratory depression in healthy patient as do ordinary pethidine. It is a good substitute for pethidine for safety reasons. Pethilorphan does not relieve respiratory depression caused by other medical condition.

ii. Non narcotic analgesics

ACETYLSALICYLIC ACID

300 mg/tab; 500 mg/cap

Acetylsalicylic acid has analgesic, anti-pyretic and anti-inflammatory action. It is one of the essential drugs because of its low toxicity, cheapness and ready availability. It is indicated in less severe pains like headache, neuralgia, gout, neuritis, rheumatic joint pains, myalgias, cold, toothache and feverish conditions. Acetylsalicylic acid acts on the hypothalamus and inhibits prostaglandin that is responsible for production of inflammation, fever and pains. Dose: 0.3-1g in divided doses for analgesic and antipyretic, 0.5-1g every 4 hours in chronic rheumatism. All by oral administration. It is contraindicated in gastric lesion, and asthma. Side effects include dyspepsia, haematemesis and melaena.

Brand name: Aspirin

PARACETAMOL

500 mg, 125 mg/tab. or cap. 125 mg/5 ml syrup or susp.

Paracetamol has analgesic action, but no anti-inflammatory effect. It is a good substitute to patients sensitive to acetylsalicylic acid. Its hepatotoxic effect is irreversible. This effect is always due to overdose. Paracetamol is used to relieve pain in conditions like Toothache, Pain During Periods, Pain associated with Arthritis, Backache, Muscle Pain, Fever, Pain, Head Pain. Migraine Headache, rheumatism and neuralgia. Do not take this medication for fever for more than 3 days. For adults, do not take this product for pain for more than 10 days (5 days in children) Pain medications work best if they are used as the first signs of pain occur. If you wait until the symptoms have worsened, the medication may not work as well. . Paracetamol causes less gastric irritation than acetylsalicylic acid and is more preferred in elderly patient. The adult dose is 0.5 to 1g every three or four hour. Children aged 3-7: 250 mg, 7-12 years: 500 mg

Popular brand name: panadol,

Non steroidal anti-inflammatory drugs

(NSAIDs) and drugs used for gout

INDOMETHACIN

25 mg/cap

This is a non-steroidal anti-inflammatory drug. It has analgesic, antipyretic and anti-inflammatory effect and is therefore used in the treatment of musculoskeletal disorders such as osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, gout, dysmenorrhoea and lumbago. A dose of 25-50 mg b.i.d or t.i.d is advised with meals. Higher doses can produce such effects like headache, nausea, vomiting, epigastric discomfort and gastric lesion. Indomethacin is contraindicated in patient with history peptic ulcer disease and asthma.

Brand name: Indocid

DIFLUNISAL

250 mg/tab

Diflunisal has about 8 to 12 hours duration of action without antipyretic effect but anti inflammatory and analgesic effect. Its major area of action is inflammatory conditions and pains like osteoarthritis, rheumatoid arthritis and pains and associated symptoms of dysmenorrhoea. The usual therapeutic dose in patients with osteo or rheumatoid arthritis is between 500 mg to 1g daily in one or two divided doses. In painful conditions like dysmenorrhoea, initial dose of 1g followed by 500 mg b.i.d is recommended. It is contraindicated in asthmatic attack, patients allergic to salicylates or other NSAIDs, gastric intestinal ulcer. Adverse effects are gastrointestinal pains, dyspepsia, nausea, tinnitus. S/P: ulcerative patients, patients receiving anticoagulant, liver diseases. Diflunisal is mostly available in tablets and should not be administered together with indomethacin.

Brand name: Dolobid

DICLOFENAC

25 mg and 100 mg per tab.

Inflammatory and degenerative form of rheumatism, acute musculoskeletal disorders, acute gout, post traumatic and post operative inflammation and pain; painful conditions of the ear, nose and throat; renal and biliary colic, dysmenorrhoea and inflammatory infections. Adult dose of 75 to 150mg daily is recommended orally or intramuscularly with food. It is contraindicated in peptic ulcer disease, asthma and pregnancy. Side effects involved are nausea, vomiting, dyspepsia, rashes, gastrointestinal pain, headache, dizziness.

Brand name: Voltaren

IBUPROFEN

200 and 400 mg per tab/cap

A non-steroidal anti-inflammatory agent indicated in the treatment of muscular and soft tissue pains, rheumatoid arthritis, osteoarthritis, analgesic and anti-inflammatory conditions. Initial dose of 1.2g daily in divided doses and maintenance dose of 600 mg daily also in divided doses. Toxic effects: gastrointestinal upset or haemorrhage skin rash. Contraindications: history of or active peptic ulcer.

Synonym: Brufen, Motrin

KETOPROFEN

500, 100 and 200 mg per cap; 100 mg/2ml amp.

Ketoprofen controls symptoms for a period of 24 hours with a central analgesic activity for a powerful pain relief. Its main area of action is rheumatological disorders, ankylosing spodylitis, acute gout, acute painful musculoskeletal conditions, cervical spondylitis, acute gout and postoperative pains. 100-200 mg daily single daily dose with food. Route of administration could either be by mouth or deep intramuscular injection. Contraindications: pregnancy, patients allergic to NSAIDs, bronchial asthma, active peptic ulcer, dyspepsia and renal dysfunction.

Synonyms: Orudis, Oruvil

NAPROXEN

250 mg, 500 mg per tab.

Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, acute gout, acute musculoskeletal disorders, dysmenorrhoea, and other painful and inflammatory conditions. 500-1000 mg daily in two divided doses at twelve hourly intervals or as a single daily dose depending on clinical reasons. S/E: skin rash, GI intolerance, headache tinnitus and vertigo. S/P: elderly, history or active gastrointestinal lesions, renal or hepatic impairment, and heart failure. C/I: NSAIDs induced allergy, active peptic ulcer, pregnancy, lactation and children.

PIROXICAM

10 and 20 mg/tab and cap. 10 mg/ml amp.

A non steroid anti-inflammatory agent for the management of osteoarthritis, rheumatoid arthritis ankylosing spondylitis, gout, muscle and skeletal disorders, dysmenorrhoea, post traumatic and post operative pains and inflammatory conditions. A standard dose of 20 mg daily as single dose for three days is advised. In acute state give 40 mg daily for 2 days then 20 mg daily for 5-12 days. In the case of gout, initial dose of 40 mg as a single dose then 40 mg daily in single or divided doses for next 4 to 6 days. Children below 15 kg: 5 mg/kg; 16-25kg: 10 mg/kg; 26-45 kg: 15 mg/kg; over 46 kg: as for adult, all as single daily dose. It is contraindicated in history of or active peptic ulcer, patient sensitive to NSAIDs, pregnancy, lactation and asthma. S/E: GI disturbance, oedema, injection site reactions, tinnitus.

Synonym: Feldene

ALLOPURINOL

100 mg/tab

Inhibit xanthine oxidase enzyme that produces uric acid. For this reason, it is useful in the treatment of gout. Initiation of therapy may be accompanied by an increase of acute gout attacks, therefore colchicines or an anti-inflammatory drug should be given concurrently when initiating therapy. Allopurinol reduces the production of uric acid by inhibiting xanthine oxidase. So allopurinol prevents the production and deposition of uric acid as sodium urate crystal in the joint, tendon sheets, and organs which in turn causes gout. It is also used in the management of calcium oxalate renal stones when fluid and dietary measures have failed. However allopurinol should only be used in chronic gout. It is on record that allopurinol should not be used in acute gout as it exacerbate and prolong symptoms. Adult dose is 100-200mg daily in mild conditions. Larger doses should be administered in divided doses of not more than 300mg/day in divided doses. C/I: aspirin, acute gout; S/P: pregnancy elderly, renal or hepatic dysfunction; S/E: Nausea and acute gout, Skin reactions (withdraw if occur). NOTE: NSAIDs should be used in the treatment of acute gout Brand name: Zyloric

1 comment:

Anonymous said...

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