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DRUG PHARMACOPOEIA

Written by Dr A I Manjra

For Health Professionals

Contents Antihistamines
Bronchodilators
Theophyllines, Oral Theophyllines
Steroids, Oral Steroid, Intravenous Steroids, Nasal Steroids, Inhaled Steroids,  Topical steroid preparations, Treatment of allergic rhinitis, Ani-allergic eye preparations

ANTIHISTAMINES

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DRUG PRESENTATION DOSE SIDE EFFECT
ADULT PAED
Chlorpheniramine maleate (Chlortrimetron, Allergex, Histamed) Tabs: 4mg
Syrup: 2.5mg/ml
Parenteral: 10mg/ml		 1 tds 0.35mg/kg/day as above
Clemastine fumarate
(Tavegyl)		 Tabs: 1mg
Syrup: 0.5mg/5mls
Parenteral: 2mg/ml		 1 bd 1m-1yr: 0.025mg/kg/
24hrs (2 divided dose)
1-4yrs 2.5-5mls bd
4-12yrs 5-10mls bd		 as above
Dexchlorpheniramine
(Polaramine)		 Tabs: 2mg
Repetabs: 6mg
Syrup: 2mg/5mls		 Tabs: 1 tds
Repetabs: 1 bd		 Infants 1.25mls tds Older children
<12yrs 2.5mls tds		 as above
Diphenhydramine
(Benadryl)		 Capsule: 50mg
Parenteral: 10mg/ml
Elixir: 12.5mg/5mls		 1 tds 5mg/kg/day Sedation
Dry mouth
Blurred vision
Hydroxyzine hydrochloride
(Aterax)		 Tabs: 10mg/25mg/100mg
Syrup: 10mg/5mls
Drops: 7.5mg/ml
Parenteral: 2mg/ml		 10-300mg/da 2mg/kg/day
Drops: 0.5-1mg/kg (Infants)		 as above
Mebhydrolin
(Fabahistin)		 Tabs: 50mg
TRT: 150mg
Suspension: 50mg/5mis		 TRT: 1 daily
Tabs: 2 p.r.n.		 <2yrs: 5mls daily
2-5yrs 5-10mls daily
5-10yrs: 15mls daily
>10yrs: adult dose		 Sedation
Dizziness
Hypotension
Weakness
Incoordination
Mepyramine maleate
(Anthisan)		 Tabs: 50mg/100mg
Inject: 25mg/ml
Elixir: 25mg/5mls		 100mg tds injection
25-50mg		 (1drop=1mg) 1mg/gk bd as above
Oxatomide (Tinset) Drops: 25mg/ml
(25drops=1ml) Tabs: 30mg		 1 bd (1 drop=1mg) 1mg/kg bd as above
Promethazine hydrochloride
(Phenergan) (Daralix)		 Tabs: 10mg/25mg
Syrup: 5mg/5mls
Parenteral 25mg/ml		 1 p.r.n. 0.5mg/kg/dose as above
LESS SEDATING ANTIHISTAMINES

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Astemizole (Hismanal) Tabs: 10mg
Syrup: 5mg/5mls		 1 daily 0.2mg/kg/dose. Once a day Headache
Dizziness
Weight gain
Cetirizine (Zyrtec) Tabs: 10mg 1 daily

-

 Headache
Dry mouth
Dizziness
Loratidine (Clarityne) Tabs: 10mg
Syrup: 5mg/5mls		 1 daily 2-12 yrs
<30kg: 5mls daily
>30kg: 10mls daily		 Dizziness
Terfenadine (Triludan) Tabs: 60mg 1 bd

-

 Dizziness
Dry mouth

BRONCHODILATORS

ß-2-AGONISTS

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See chapters 10, 11 and 12

Side Effects of ß-2-Agonists

Tremor, Tachycardia, Palpitations, Headaches, Hypokalaemia and Hyperglycaemia

DRUG PREPARATION DOSE
ADULT PAED
Fenoterol (Berotec) Oral Tab: 2.5mg
Syrup: 2.5mg/ml		 2.5mg tds 2.5mg tds
MDI:
Inhalets:		 100µg/puff
200µg/tablet		 2 puffs tds 1-2 puff tds
Nebulised Solution 1mg/ml
UDV Paed
        Adult
1.25mg
0.5mg		 1-2mls/dose 0.5-1mls/dose
Formoterol fumarate
(Foradil)		 Inhaler 1 puff bd 1 puff bd
Hexoprenaline (Ipradol) Oral tabs: 0.5mg
Syrup: 125mg/
5mls		 0.5-2 tab tds (also
sublingual)		 3-6 months 5mls
daily 6-12 months
1-3yrs 5-10mls 1-3X daily >3-10mls 1-3X daily
Injection 2.5µg/ml (2ml amp) STAT 2mls
IVI slowly over 5mins. Maintenance 100-300µg/l in 5% dextrose. Give 0.3-0.45 µg/min.		 3-6months: 1µg as infusion.
6-12months: 2µg as infusion.
1-3yrs: 2-3µg as infusion. >3yrs 3-4µg as infusion.
Nebulisation 250µg/ml Mix with equal volume of normal saline (use every 6 hrly)
Aerosol 0.1µg/dose 1-2 puffs 6hrly 1-2 puffs 6 hrly
Salbutamol (Ventolin, Venteze) Tabs: 2mg/4mg, Syrup: 2mg/5mls oral dose 2-4 tds or qid 2-6yrs 0.5mg/kg/tds
(max 2mg tds)
6-12yrs 2mg tds
MDI : 100µg/puff
Rotacaps 100 and 200µg		 Inhaled dose 2 puffs every 4-6 hrs as needed 2 puffs every 4-6
hrs as needed
Ventodisc 200µg & 400µg   200-400µg/dose
4-6 hrly		 200µg 4-6 hrs
Nebulised Solution 0.5% solution Nebules 2.5mg & 5mg   5mg/dose 0.01-0.03ml/kg in 2ml normal saline or use 2.5mg nebules 3-6 hrly
IV
0.5mg/ml-1mg/ml		 1ml 20µg/kg 20µg/kg
Long-acting Salbutamol
(Volmax)		 4mg/8mg 4-8mg bd 0.6mg/kg/day divided by 2 dose
Salmeterol (Serevent)
MDI:
Disk:
25µg/actuation
50µ/blister
2 puffs bd
1 disc bd
2 puffs bd
1 disc bd

THEOPHYLLINES

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Factors Altering Serum Theophylline Levels

FACTOR INCREASED DECREASED
Age 1-16yrs Prematurity
Neonates
Elderly
Weight   Obesity
Diet   High carbohydrate
Braai meat
Habits   Cigarettes
Drugs Phenobarb
Phenytoin
Rifampicin		 Cimetidine
Macrolide antibiotics
Propanolol
Oral contraceptives
Quinolones
INH
Ranitidine
Diseases Cystic Fibrosis
Hyperthyroidism		 Liver disease
CCF
Pneumonia
Viral infections
Alcoholism
Therapeutic Serum Theophylline levels 10-20µg/ml of Blood

Side Effects of Theophyllines

Nausea, Vomiting, Abdominal pain, Headache, Insomnia, Anxiety, Enuresis, Restlessness.

ORAL THEOPHYLLINES

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DRUG PREPARATION DOSE
ADULT PAED
Etophylline, equivalent to 80mg theophylline
(Theostat)		 Syrup: 80mg/5mls Tab: 100, 200mg 30-45mls 6 hourly 100-200mg bd 2-8yrs: 15-30ml/dose
9-10yrs: 30-40ml dose. 20-24mg/kg/day.
Aminophylline
(Peterphylline)		 100, 200mg tablets 1-2 tab prn 5mg/kg/dose
Theophylline anhydrous
(Microphylline)		 60, 125, 250mg capsules 250-500mg bd 2-6yrs: 60-125mg bd
6-12yrs: 125-250mg bd
Theophylline anhydrous
(Nuelin SA)		 250mg 1-2 tabs bd 20-24mg/kg/day
Theophylline
(Nuelin liquid)		 Theophylline
25mg/5mls		 18mg/kg/day divided by 4 dose <1yr 2.5mg/kg/dose 6hrly.
>1yr 5mg/kg/dose
Theophylline anhydrous
(Theodur)		 200,300mg tablets <35kg/200mg bd
>35kg/300mg bd.
Up to 450mg bd		 20-24mg/kg/day
Theophylline anhydrous
(Theoplus)		 200, 300mg 100-300mg bd 20-24mg/kg/day
divided by 2
Theophylline ethylenediamine (350mg)
(Euphylline retard)		 Equivalent:
280µg theophylline		 1 bd 20-24mg/kg/day
INTRAVENOUS AMINOPHYLLINES
DRUG PREPARATION DOSE
ADULT PAED
Aminophylline 500mg/2mls
250/10mls		 250mg-500mg
slowly IVI
1 ml/min		 Load 6mg/kg IVI over 20min. thereafter for constant infusion 0.5-1mg/kg/hr
ANTI-CHOLINERGICS
DRUG/PREPARATION DOSE SIDE EFFECT
ADULT PAED
Ipratropium bromide
(Atrovent)
Inhaler 40µg/inhalation.
Inhalets: 40µg
Nebulised -
Paed: UDV 0.25mg
Adult: UDV 0.5mg

both

1-2 puffs 6-8hrly
1 capsule tds

1 dose tds or qid
1 dose tds or qid

 Dry mouth
Tachycardia
Face flushin
Blurred vision
NON-STEROIDAL ANTI-IMFLAMMATORY DRUGS
Ketotifen
(Zaditen)
Tablet:1mg
Slow release
Tablet: 2mg
Syrup: 1mg/5mls		 1 tablet bd
Slow release
tab daily		 <14ky 1.5mls bd
14-25kg/2.5ml bd
>25kg/5ml bd		 Sedation
Dry mouth
Dizziness
Sodium cromoglycate
(Lomudal)
Spincaps: 20mg/cap
MDI: 1mg and 5mg
Nebulised
Solution: 20mg/vial

both

1 qid (can reduce to tds)
2-10mg qid (can reduce to tds)
1 vial 6hrly

 No side effects

STEROIDS

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Guideline for Oral Steroids

  1. Use agents with short duration of action.

  2. If possible use topical steroids i.e. creams for eczema and inhaled steroids for respiratory allergy.

  3. Use lowest dose that controls the disease.

  4. Avoid long courses. Limit the duration to 5-10 days. No tapering is required if using for a short duration.

  5. Use single doses rather than divided since single doses have less adrenal suppression.

  6. If long courses are needed, comsider using alternate day steroid use.

  7. Do not abruptly stop high dose long term steroid therapy. Doing so can precipitate the underlying disease or cause adrenal insufficiency. Gradually wean patients off prolonged steroid therapy.

Reduce by 2.5-5mg of prednisone every 3days. Observe disease activity. If asthma exacerbates increase the dose and try to reduce gradually if no exacerbation occurs. Wean to 5mg of prednisone/try then gradually stop.

Side effects of Steroids

  1. General: Cushings appearance, Increased appetite, Weight gain, Growth suppression, Hyperglycaemia, Hyperlipidaemia.

  2. CVS: Hypertension, Arthritis, Arrhythmia, CCF, Oedema.

  3. CNS: Mood swings, Insomnia, Headache, Psychosis.

  4. Bone: Osteroporosis, Aseptic necroses.

  5. Endocrine: Suppression HPA axis.

  6. GIT: Peptic ulcers, Pancreatitis.

  7. Blood: Coagulation defects.

  8. Immune: Suppress Immunity.

  9. Ocular: Post subcapsular cataracts.

  10. Skin: Acne, Purpura, Thinning of skin, Striae, Hirsutism, Telangiectasia.

 

ORAL STEROIDS
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DRUG PREPARATION DOSE FOR ASTHMA
IN CHILDREN*
SHORT ACTING:
(Meticortelone)
Methylprednisolone
(Medrol)
tabs: 4mg, 16mg
1-2mg/kg/day
Prednisolone
(Predeltilone)		 tabs: 5mg 1-2mg/kg/day
Prednisolone syrup
(Prelone)		 15mg/5mls 1-2mg/kg/day
Prednisolone
(Meticorten,
Panafort, Predeltin)		 tabs: 5mg 1-2mg/kg/day
LONG ACTING:
Betamethasone
tabs: 0.5mg
syrup: 0.6mg/5mls
0.5-6mg/day
Child dose depending on severity.
Dexamethasone tabs: 0.5mg 0.6mg/kg/dose
INTRAVENOUS STEROIDS
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DRUG PREPARATION DOSE
Hydrocortisone
(Solu-cortef)
 100mg/2mls
500mg/4mls		 4mg/kg every 4-6hrs
Methyprednisolone
(Solu-Medrol)		 40mg/mls
125mg/2mls
500mg/8mls
1g/16mls		 1-2mg/kg every 6hrs
(can use higher dose)
For adult doses consult Chapter 12

NASAL STEROIDS
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DRUG PREPARATION DOSE
Beclomethasone
dipropionate
(Beconase, Viarox,
Clenil, Ventnase)		 50µg/actuation 1-2 puffs bd
Budesonide
(Rhinocort)		 50µg/dose
Daily aqueous:
100µg/dose		 1-2 puffs bd
or daily dose
Flunisolide
(Syntaris)		 25µg/actuation 1-2 puffs bd
Fluticasone
propionate

(Flixonase)

 25µg/dose 1-2 puffs once a day
Triamcinolone
acetonide
(Nacasor)		 55µg/actuation 1-2 puffs daily
(adults only)

INHALED STEROIDS
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DRUG PREPARATION DOSE
Beclomethasone
dipropionate
(Becotide)		 MDI: 50,100,250µg/inhalation.
Becloforte = 250µg/inhalation
Rotacaps 100 & 200µg/capsule
Becodisc 100µg/200µg		 100-600µg/day in divided doses
Generics
(Viarox, Ventzone
& Clenil)
MDI: 50µg/inhalation.
Dipropionate MDI		  
Budesonide
(Pulmicort)
Generic
(Inflammide)		 Pulmicort turbuhalers
100µg/200µg
Pulmicort MDI: 50,100,200µg
Inflammide MDI: 50,100,200µg		 100-600µg/day in divided doses
Fluticasone
propionate
(Flixotide)		 MDI: 25,50,125,250µg
Disc: 50,100,250,500µg		  

*For detailed dosing schedules, consult Chapters 10, 11 and 12.

Guidelines for Topical Steroid use in Eczema.

These preparations are available as fluorinated and non-fluorintaed compounds. The fluorinated compounds have anti-inflammatory effects as well as side effects when compared with the non-fluorinated group.
However some non-fluorinated compounds are potent as well.

  1. Creams are used for wet lesions. Ointments for dry lesions. Lotions are useful for scalp lesion.

  2. Emollients can be applied over topical steroid.

  3. Avoid as far as possible very potent steroids in children. These should NEVER be used on the face. Most infants will respond favourably to the mild and moderately potent steroid.

  4. Adrenal suppression can occur if more than 50g/week (adults) or 10mg/week (children) if a very highly potent steroid is applied.

  5. Only 0.5-1% hydrocortisone should be used on the face.

Side Effects of Topical Steroids

Skin atrophy, Striae, Hypopigmentation, Acne, Hypertrichosis, Telangiectasia, Burning, Itching.

TOPICAL STEROID PREPARATIONS*

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VERY POTENT
Flucinolone acetonide
Clobetasol propionate
Betamethasone dipropionate
0.2%
0.05%
0.05%
Synalar forte
Dermovate
Diprosone (Diprolene)
POTENT
Betamethasone valerate
Flucinolone acetonide
Diflucortolone valerate
Hydrocortisone butyrate
0.1%
0.025%
0.1%
0.1%
Betnovate
Synalar (Cortoderm)
Nerisone
Locoid
MODERATELY POTENT
Clobetasone butyrate
Mometasone furoate
Fluticasone propionate
0.05%
Eumovate
Elocon
Cutivate
LOWEST POTENCY
Hydrocortisone
Hydrocortisone
1%
0.05%
Procutan/Mylocort
Dilucort/Cutaderm
Skincalm

See also Chapter 8 for further guidelines.

TREATMENT OF ALLERGIC RHINITIS
NON-STEROID NASAL PREPARATIONS

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DRUG PREPARATION DOSE
Levocabastine
(Livostin)		 0.5 mg/ml 2 puffs bd
Na cromoglygate
(Rynacrom)
(20mg/ml)		 Spray: 20mg/ml
Drops: 20mg/ml
0.8mg/drop		 1 dose qid in each nostril

 

ANTI-ALLERGIC EYE PREPARATIONS

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DRUG PREPARATION DOSE
Levocabastine
(Livostin)		 Drops 5mg/ml 1 drop bd.
Na cromoglycate
(Opticrom)		 Drops 20mg/ml
Ointment 200mg/5mls		 1-2 drops
4 x daily in each eye.

 

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