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Havard's Nursing Guide to Drugs, 8th Edition - Adrianna P. Tiziani
Havard's Nursing Guide to Drugs, 8th Edition - Adrianna P. Tiziani
Havard's Nursing Guide to Drugs, 8th Edition - Adrianna P. Tiziani
Havard's Nursing Guide to Drugs, 8th Edition - Adrianna P. Tiziani
Havard's Nursing Guide to Drugs, 8th Edition - Adrianna P. Tiziani
Havard's Nursing Guide to Drugs, 8th Edition - Adrianna P. Tiziani
Havard's Nursing Guide to Drugs, 8th Edition - Adrianna P. Tiziani
Havard's Nursing Guide to Drugs, 8th Edition - Adrianna P. Tiziani
Havard's Nursing Guide to Drugs, 8th Edition - Adrianna P. Tiziani
Havard's Nursing Guide to Drugs, 8th Edition - Adrianna P. Tiziani
Havard's Nursing Guide to Drugs, 8th Edition - Adrianna P. Tiziani
Havard's Nursing Guide to Drugs, 8th Edition - Adrianna P. Tiziani
Havard's Nursing Guide to Drugs, 8th Edition - Adrianna P. Tiziani
Havard's Nursing Guide to Drugs, 8th Edition - Adrianna P. Tiziani
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Havard's Nursing Guide to Drugs, 8th Edition - Adrianna P. Tiziani

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Havard’s Nursing Guide to Drugs 8e is an essential resource for all nursing students and practitioners. The information presented in this user-friendly guide can be accessed either by therapeutic …

Havard’s Nursing Guide to Drugs 8e is an essential resource for all nursing students and practitioners. The information presented in this user-friendly guide can be accessed either by therapeutic class or by system. Each section is introduced by a clear description, followed by the A-Z of drugs within the given therapeutic class. It includes the action, use and dosage of each drug as well as important nursing points and nursing cautions. This comprehensive guide includes both trade and generic drug names for the reader’s ease of use. As with previous editions of Havard’s Nursing Guide to Drugs each drug is independently reviewed with obsolete drugs being removed and new drugs added. Each existing drug is also independently examined so as to ensure that its use, doses, side effects, contraindication and precautions comply with that of the Therapeutic Goods Association (TGA).
Key Features

* slotted lift out card contains calculation formulae and selected abbreviations
* pocket-sized format for greater portability
* systematic update of all drugs throughout the book
* available forms will be added to each drug entry
* new Appendix for Normal Blood Values will be included with the eighth edition

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  • 1. ANTI-PARKINSON’S AGENTS In 1817 James Parkinson described what • non-pharmacological (treatment of would become known as Parkinson’s symptoms); or disease. Parkinson’s disease results from • surgical (lesioning involves destroying degeneration of the dopaminergic neurons small areas of brain tissue responsible in the substantia nigra, leading to decreased for abnormal activity. Deep brain dopamine concentrations in the brain. stimulation uses electrical stimulation Symptoms of parkinsonism become evident to interfere with abnormal activity. A when more than 80% of the neurons have number of other procedures including degenerated. The cause of Parkinson’s cell transplantation with stem cells are disease is unknown although some drugs, still in the experimental stages). particularly the antipsychotic agents, are Pharmacological treatment for Parkinson’s known to induce parkinsonian symptoms. disease involves a number of different classes Other causes include encephalitis, trauma, of agents, however none actually stops the stroke, neurotoxins, other neurological progression of the disease. These pharmaco- disorders or, rarely, a genetic predisposition logical agents aim at reducing the symptoms (although early onset Parkinson’s disease is to a manageable level and include: thought to run in families) (Rang, Dale, • dopaminergic agents Ritter and Flower, 2007). Symptoms include – levodopa (precursor to dopamine) difficulty starting to walk (and once started, – dopamine agonists (e.g. apomorphine, difficulty stopping or changing directions), bromocriptine, cabergoline, pergolide) a shuffling gait, inability to perform skilled – amantadine (antiviral agent which has tasks, a blank facial expression, impairment dopaminergic activity) of speech, muscle rigidity, slow initiation of • catechol-O-methyl transferase (COMT) movement and a resting tremor. inhibitors (e.g. entacapone) Treatment for Parkinson’s disease may • monoamine oxidase type B enzyme be: (MAO-B) inhibitors (e.g. selegiline) • pharmacological (based on restoring the • anticholinergics (e.g. benztropine, benz- supply of dopamine to the brain); hexol, biperiden). ANTICHOLINERGIC ANTI-PARKINSON’S AGENTS Action Adverse effects • inhibit the action of acetylcholine at the • nausea, vomiting, dry mouth, constipation muscarinic receptors of the parasympathetic • dizziness, drowsiness, weakness, headache, division of the autonomic nervous system nervousness, euphoria, excitement • reduce production of sweat, saliva, • anhidrosis lacrimal, nasal, bronchial, gastric and • tachycardia intestinal secretions • urinary urgency, difficulty and retention • reduce GI tone and gastric acid pro- • mydriasis, photophobia, cycloplegia, duction blurred vision, raised intraocular pressure, • increase heart rate by blocking vagal dry eyes stimulus • neuroleptic malignant syndrome-like • raise intraocular pressure reaction (abrupt dose reduction or • inhibit micturition discontinuation) • mydriasis, cycloplegia • (rare) parotitis, rash, dilatation of colon, Use paralytic ileus, delusions, hallucinations • all types of parkinsonism (adjunct) Interactions • prevention of drug-induced extrapyramidal • if given with levodopa, doses of one or symptoms both agents may need to be reduced 348
  • 2. ANTI-PARKINSON’S AGENTS • may increase dopaminergic effects of physical exercise or manual work in hot levodopa environments due to decreased sweating • increased risk of tardive dyskinesia if and the risk of overheating and heat stroke given with other anticholinergic or • patient should be advised to immediately antipsychotic agents report any fever, heat intolerance or • may decrease effects of metoclopramide GI problems (especially if also taking • additive anticholinergic effects (including phenothiazines, haloperidol or other risk of paralytic ileus) may occur if given anticholinergic agents) with other anticholinergic agents or • not recommended for tardive dyskinesia MAOIs/TCAs with anticholinergic alone or for prevention of drug-induced properties parkinsonism • increased renal tubular absorption, • caution if given to those with a history decreased excretion and increased of seizures, arrhythmias, heart failure, effects may occur if given with carbonic coronary heart disease, mitral valve anhydrase inhibitors stenosis or hypertension • not recommended with alcohol • caution if given to those with liver or • increased sedation may occur if given kidney impairment, prostatic hypertropy with alcohol, hypnotics, sedatives and or obstructive GI disease other CNS depressants • caution if used during fever, high Nursing points/Cautions environmental temperatures, during • if dry mouth is problematic, may be taken physical exercise or those doing manual before meals or if nauseous, may be taken work in hot environments because of after or with meals decreased sweating • thirst may be relieved by water, chewing • contraindicated in those with narrow- gum or mints, or sucking hard sweets angle glaucoma or tardive dyskinesia • patient should be advised to avoid alcohol not recommended during preg- • patient should be advised to avoid nancy or breastfeeding unless sudden withdrawal of the drug as it benefits outweigh potential may precipitate a syndrome similar to risks neuroleptic malignant syndrome (hyper- pyrexia, muscle rigidity, psychological BENZHEXOL (Artane) changes, increased serum creatine phos- phokinase) which is potentially life Available forms threatening Tablets: 2 mg, 5 mg • advise patient to avoid driving or Dose operating heavy machinery if blurred vision, dizziness or drowsiness occurs ▪ (parkinsonism) initially 1 mg orally before or with food, increasing by 2 mg increments • intraocular pressure should be monitored at 3–5-day intervals to 6–10 mg daily (in 3 regularly divided doses) according to response. May • patient should be advised to report any require 12–15 mg in advanced cases (in blurring of vision 4 divided doses with meals and at bedtime) OR • dark glasses should be worn if there is continuous mydriasis and cycloplegia ▪ (drug-induced parkinsonism) initially 1 mg orally daily, increasing dose gradually to • patients who wear contact lenses should 5–15 mg orally daily in divided doses until be advised to use lubricating drops more symptoms are controlled frequently during therapy Adverse effects • patients should be advised to avoid high environmental temperatures, doing ▪ see general Adverse effects for anticholin- ergic anti-Parkinson’s agents 349
  • 3. HAVARD’S NURSING GUIDE TO DRUGS Interactions Interactions ▪ increased risk of euphoria if given with ▪ caution if given with ketoconazole large amounts of caffeine ▪ increased reduction of GI motility and ▪ effects may be decreased if given with cit- rus and fruit juices bladder function may occur if given with opioid antagonists ▪ additive effects may occur if given with cannabis, barbiturates, opioid analgesics or ▪ actions may be antagonised by parasympa- thomimetic agents (e.g. acetylcholine) alcohol (increasing risk of abuse) ▪ see also general Interactions for anticho- ▪ decreased blood levels may occur if given with alcohol linergic anti-Parkinson’s agents Nursing points/Cautions ▪ decreased absorption may occur if given with magnesium hydroxide ▪ parenteral administration may provide quick results if patient is psychotic with ▪ may decrease seizure control if given with antiepileptic agents acute dystonic reactions ▪ increased risk of dry mouth, blurred vision ▪ some patients may benefit from taking entire dose at bedtime (i.e. enable them and urine hesitancy if given with memantine to roll over in bed independently) whereas ▪ see general Interactions for anticholinergic anti-Parkinson’s agents others prefer divided daily doses Nursing points/Cautions ▪ (drug-induced parkinsonism) therapy should be stopped after 1–2 weeks to ▪ patient should be advised against ingesting determine if continued use is necessary large amounts of caffeine or fruit/citrus juices and to avoid alcohol during therapy ▪ see also general Nursing points/Cautions for anticholinergic anti-Parkinson’s agents ▪ should be separated by at least 2 hours from magnesium hydroxide (antacid) BIPERIDEN (Akineton) ▪ see also general Nursing points/Cautions for anticholinergic anti-Parkinson’s agents Available forms Tablets: 2 mg BENZTROPINE (Benztrop, Cogentin) Use ▪ see general uses of anticholinergic agents Available forms ▪ pyramidal spasticity Tablets: 2 mg; Ampoules: 2 mg/2 mL ▪ closed craniocerebral trauma and post- concussion symptoms Action ▪ nocturnal leg-muscle cramps ▪ has both anticholinergic and antihistamine ▪ trigeminal neuralgia actions Dose ▪ combination of active portions of atropine (see Anticholinergic agents) and diphen- ▪ (parkinsonism) initially 1 mg orally twice daily, gradually increasing to 1–4 mg orally hydramine (see Antihistamines) 3–4 times daily OR Dose ▪ (drug-induced extrapyramidal symptoms) ▪ (arteriosclerotic or idiopathic parkinson- ism) initially 0.5–1 mg orally or IM, increas- 1–2 mg orally 1–4 times daily, increasing if required (daily maximum 18 mg) (together ing dose gradually at 0.5 mg increments with an antipsychotic drug) OR and 5–6-day intervals (daily maximum ▪ (pyramidal spasticity) initially 1 mg orally 2–3 times daily, increasing gradually to 6 mg) OR ▪ (drug-induced parkinsonism) 1–4 mg orally 4 mg orally 3 times daily OR or IM 1–2 times daily OR ▪ (closed craniocerebral trauma and post- ▪ (emergency, acute dystonic reaction) 1–2 mg IM or IV stat, repeated if required concussion symptoms) 2–4 mg orally 3 times daily, for 5–9 weeks OR Adverse effects ▪ (nocturnal cramps) 4 mg orally nightly for 10–30 days OR ▪ see general adverse effects for anticholin- ergic anti-Parkinson’s agents ▪ (trigeminal neuralgia) 2–4 mg orally 3 times daily for at least 60 days 350
  • 4. ANTI-PARKINSON’S AGENTS Adverse effects ▪ may increase CNS adverse effects of pethi- ▪ see general Adverse effects for anticholin- dine ergic anti-Parkinson’s agents ▪ increased dyskinesia may occur if given with levodopa Interactions ▪ increased CNS/peripheral adverse effects ▪ see also general Interactions for anticho- linergic anti-Parkinson’s agents may occur if given with antihistamines or spasmolytic agents Nursing points/Cautions ▪ may increase antipsychotic-induced tardive dyskinesia ▪ see also general Nursing points/Cautions for anticholinergic anti-Parkinson’s agents CATECHOL-O-METHYL TRANSFERASE (COMT) INHIBITORS ENTACAPONE (Comtan) ▪ may increase bioavailability of levodopa, increasing the risk of dopaminergic Available forms adverse effects Tablets: 200 mg ▪ contraindicated with non-selective or selective MAOIs (except selegiline at Action doses less than 10 mg) ▪ inhibits COMT in peripheral tissues, reducing metabolism of levodopa by ▪ high doses may decrease bioavailability of carbidopa COMT, increasing the amount of levodopa and therefore the amount of dopamine ▪ may increase serum levels of warfarin, increasing the risk of bleeding, therefore Use INR should be monitored closely especially ▪ Parkinson’s disease as an adjunct to when starting, stopping or altering dose levodopa to control motor fluctuations ▪ not recommended with TCAs, nor- adrenaline reuptake inhibitors, isoprena- Dose line, adrenaline, noradrenaline, dopamine, ▪ 200 mg orally (with levodopa–carbidopa or levodopa–benserazide) 4–7 times daily dobutamine, methyldopa, apomorphine or paroxetine (maximum daily dose 2 g) ▪ may increase the risk of dopaminergic Adverse effects effects including dyskinesia if given with ▪ diarrhoea, nausea, vomiting, dry mouth, abdominal pain, constipation dopamine agonists, selegiline or amanta- dine ▪ dizziness, drowsiness, fatigue, headache, vertigo, insomnia, daytime somnolence, Nursing points/Cautions sudden sleep onset ▪ should be taken 2–3 hours apart from meals to prevent chelation with dietary iron ▪ falls, pain, back pain, leg cramps ▪ levodopa dose is usually reduced by ▪ dyskinesia, dystonia, tremor, aggravated Parkinson’s, hyper/hypokinesia 10–30% by either decreasing dose or increasing dosing interval ▪ hallucinations, depression, confusion, para- noia ▪ if diarrhoea is ongoing, weight should be monitored to prevent excessive loss ▪ discoloured urine, increased sweating ▪ drowsiness is a problem at the start of ▪ (rare) rhabdomyolysis, neuroleptic malig- nant syndrome therapy ▪ patient should be advised not to drive or Interactions operate machinery if drowsiness, day time ▪ may form chelates with dietary iron somnolence, sudden sleep onset or dizzi- ▪ may increase levodopa-induced or antihy- ness continues pertensive-induced hypotension ▪ family/carers should be asked to observe ▪ may require adjustment of other anti- Parkinson’s medication to decrease risk of for any sudden sleep onset as patients are often unaware that this occurs and it may dyskinesia be dangerous if the person drives or oper- ates machinery 351
  • 5. HAVARD’S NURSING GUIDE TO DRUGS ▪ patient should be advised to avoid sud- den withdrawal of the drug as it may pre- intolerance, glucose/galactose malab- sorption or sucrose/isomaltase insuffi- cipitate a syndrome similar to neuroleptic ciency malignant syndrome (hyperpyrexia, muscle ▪ contraindicated in those with liver impair- ment, phaeochromocytoma, previous his- rigidity, psychological changes, increased serum creatine phosphokinase) which is tory of neuroleptic malignant syndrome or potentially life threatening rhabdomyolysis (non-traumatic) ▪ patient should be warned that urine may contraindicated during preg- appear a harmless reddish-brown colour nancy or breastfeeding ▪ levodopa dose will require adjustment ▪ advise patient to avoid postural hypoten- Note sion by moving gradually to a sitting or ▪ combined with levodopa and carbidopa in Stalevo standing position, especially after sleep ▪ tablets contain sucrose and therefore are not recommended in those with fructose DOPAMINE AGONISTS Adverse effects Nursing points/Cautions • nausea, vomiting, constipation, dyspepsia, • before starting therapy, patients should dry mouth, weight decrease, altered taste have a cardiovascular assessment (includ- • dizziness, somnolence, hallucinations (visual, ing ECG), ESR, lung function test, chest auditory), confusion, abnormal dreams, X-ray and renal function insomnia, headache, asthenia, fatigue, • ECG should be monitored within malaise 3–6 months of starting therapy, then • postural hypotension, syncope, peripheral 6–12-monthly oedema • patient should be advised to immediately • rash, pruritus, increased sweating report any shortness of breath, persistent • dyskinesia cough or chest pain (pulmonary fibrosis) • (rare) somnolence, sudden sleep onset, or loin/flank pain, lower limb swelling or neuroleptic malignant syndrome (on abdominal tenderness (retroperitoneal abrupt withdrawal) fibrosis) • (uncommon, high doses) compulsive • chest X-ray and ESR are recommended behaviours including pathological gambl- if patient develops any pulmonary ing, increased libido, hypersexuality, symptoms shopping, eating, repetitive purposeless • drowsiness is a problem at the start of activity (punding) therapy Interactions • dose may require adjusting if given with • not recommended with agents that other anti-Parkinson’s agents antagonise dopamine receptors (e.g. • advise patient to avoid postural hypo- metoclopramide, phenothiazines, butyr- tension by moving gradually to a sitting ophenones, thioxanthines) or standing position, especially after • hypotensive effect may be enhanced by sleep antihypertensive agents • patient should be advised not to drive • caution if given with alcohol and other or operate machinery if drowsiness, day CNS depressing agents time somnolence, sudden sleep onset or • increased risk of dyskinesia, hallucinations dizziness continues and confusion if given with levodopa • family/carers should be asked to observe for any sudden sleep onset as patients 352
  • 6. ANTI-PARKINSON’S AGENTS are often unaware that this occurs and it Dose may be dangerous if the person drives or ▪ (Parkinson’s disease) initially 100 mg orally daily for 1 week, then increasing to 100 mg operates machinery • patients should be advised to avoid orally twice daily OR alcohol ▪ (drug-induced extrapyramidal effects) ini- tial treatment should be dosage reduction • observe patient for suicidal tendencies or of the drug causing the effects. If this is depression not practical then 100 mg orally 2–3 times • advise patient to discuss taking any daily, discontinuing when symptoms have OTC preparations with the doctor or been controlled pharmacist Adverse effects • patient should be advised to avoid ▪ palpitations sudden withdrawal of the drug as it ▪ mottling of skin (livedo reticularis) may precipitate a syndrome similar to ▪ blurred vision (transient), slurred speech neuroleptic malignant syndrome (hyper- ▪ (rare) urinary retention pyrexia, muscle rigidity, psychological ▪ see general Adverse effects for dopamine agonists changes, increased serum creatine phos- phokinase) which is potentially life Interactions threatening ▪ caution if used with sympathomimetic agents (e.g. phenylephrine, pseudoephed- • advise patient to resume physical activity gradually to avoid injury rine) • caution if used in those with epilepsy, ▪ increased risk of neurotoxicity and arrhyth- mias if given with antipsychotic agents confusion, psychosis, hallucinations, gastric ulcers, cardiovascular disease, ▪ see general Interactions for dopamine ago- nists congestive heart failure, postural hypotension, narrow-angle glaucoma, Nursing points/Cautions prostatic enlargement, kidney or liver ▪ advise patient to consult the doctor imme- diately if any rash appears or pregnancy impairment or history of eczema occurs not recommended in preg- ▪ see general Nursing points/Cautions for nancy or during breastfeed- dopamine agonists ing unless benefits outweigh contraindicated during preg- potential risks nancy AMANTADINE (Symmetrel) APOMORPHINE (Apomine Injection, Apomine PFS) Available forms Capsules: 100 mg Available forms Action Ampoules: 20 mg/2 mL, Prefilled syringes: 50 ▪ thought to stimulate the synthesis and release of dopamine (and other catecholamines) in mg/10 mL Action the brain and also delay reuptake ▪ dopamine agonist acting on D1 and D2 ▪ some anticholinergic activity receptors ▪ (influenza) probably inhibits penetration of the virus (influenza A) into the host cell ▪ induces vomiting by stimulating chemore- ceptor trigger zone in the medulla Use ▪ (SC) onset of action within 5 minutes, ▪ Parkinson’s disease (not indicated for tar- dive dyskinesia) elimination half-life is approximately 33 minutes ▪ drug-induced extrapyramidal reactions Use ▪ prophylaxis against influenza type A (see Antiviral agents) ▪ reduction in severity and number of motor fluctuations in Parkinson’s disease 353
  • 7. HAVARD’S NURSING GUIDE TO DRUGS refractory to other conventional treat- orally 3 times daily or less if renal insuf- ment (‘off’ phase of the ‘on–off’ phe- ficiency exists), may be reduced by 10 mg nomenon, in which the patient fluctuates daily at weekly intervals until mild nausea between mobility and immobility) reappears and may be withdrawn after sev- Dose eral weeks ▪ threshold dose (considered to be the low- ▪ antiparkinsonian medications are stopped to provoke the ‘off’ phase (immobility) est dose that produces an ‘unequivocal’ after at least 3 days hospitalisation motor response compared with baseline) ▪ after immobility has been provokedbeen and ▪ perform baseline motor assessment (unilat- eral alternate hand tapping for 30 seconds, baseline motor assessment has time to walk 12 metres, clinical assessment completed, initially 1.5 mg SC then observe of tremor and dyskinesia (4 point score) the patient for 30 minutes for motor and modified Webster disability scale to response. If there is no/poor response assess 12 features of parkinsonism (maxi- after 40 minutes, give 3 mg SC and observe mum disability score 36)). Positive motor patient for another 30 minutes. Give a third response consists of 15% increase in hand dose of 5 mg and a fourth dose of 7 mg at tapping, 25% increase in walking time, 2 40-minute intervals, if required, observing point increase in tremor score or Webster the patient for 30 minutes as previously score increase of 3 or more points (if still no response, patient is thought to be a ‘non responder’. A 10 mg dose ▪ dose for treatment may be further adjusted to response if needed can be given if the patient had a minimal response at 7 mg) ▪ patient should be advised against driving or operating machinery if somnolence, Treatment drowsiness or sudden sleep onset epi- ▪ (restarting threshold dose (as established administer antiparkinsonian treatment) sodes occur above) SC at first sign of ‘off’ phase (maxi- ▪ SC administration sites are usually the thigh and lower abdomen mum daily dose 50 mg) and observe for 1 hour OR ▪ patient/carer should be educated regard- ing injection technique, importance of site ▪ initially 1 mg/hour by continuous SCpump, sion via portable syringe driven infu- rotation, correct storage information and safe disposal of used needles increasing as necessary to achieve motor response during waking hours (maximum ▪ prefilled syringe does not require any further dilution. Ampoule is diluted using daily dose 200 mg) sodium chloride 0.9% for use in portable Adverse effects syringe-driven pump ▪ (injection site) itchy, nodular lesions, local ▪ continuous SC infusion via mini-pump may be recommended for patients who require bruising, fibrosis, necrosis ▪ eosinophilia, haemolytic anaemia more than 10 injections per day or whose ▪ see general Adverse effects for dopamine overall control is not satisfactory agonists ▪ continuous SC infusion is only required during waking hours Interactions ▪ Coombs’ positive haemolytic anaemia may ▪ infusion sites should be rotated every 12 hours occur if used in conjunction with levodopa ▪ tetrabenazine, metoclopramide, pheno- ▪ liver, kidney, blood and heart function should be regularly monitored during thiazines, thioxanthenes, butyrophenones, therapy amphetamines and papaverine should be avoided ▪ contains sodium metabisulfite, which may cause allergic reaction ▪ see general Interactions for dopamine ago- nists ▪ opioid antagonist (e.g. naloxone) may be used to treat overdosage, respiratory or Nursing points/Cautions CNS depression or excessive vomiting ▪ patient must be hospitalised during pre- ▪ prefilled syringe should be discarded 24 hours after opening treatment phase ▪ domperidone (antiemetic) is started ▪ caution if used in those with predisposi- tion to nausea/vomiting, at increased risk 48–72 hours before treatment (20 mg 354
  • 8. ANTI-PARKINSON’S AGENTS of respiratory depression or those with Use endocrine, pulmonary or cardiovascular ▪ Parkinson’s disease disease ▪ preventing or suppressing lactation, hyper- ▪ contraindicated in those with known hypersensitivity to sodium metabisulfite, prolactinaemia (see Pregnancy, childbirth and breastfeeding) morphine or related products, dementia or pre-existing neuropsychiatric problems, ▪ adjunctive therapy in acromegaly liver/kidney impairment, unstable coronary Dose vascular disease, cerebrovascular disease, ▪ (Parkinson’s disease) initially 1.25 mg orally 1–2 times daily with food for 7 days, then respiratory or CNS depression or in those with Parkinson’s disease in which the ‘on’ increasing by 1.25 mg at weekly intervals response to levodopa is marred by severe until therapeutic response is reached dyskinesia, hypotonia or psychotoxicity (range 5–40 mg) OR not recommended during preg- ▪ (adjunctive therapy in acromegaly) initially 1.25 mg orally at night increasing gradually nancy or breastfeeding over 7–14 days to 10–30 mg in 4 divided doses with food (maximum daily dose 40 BENSERAZIDE mg) Adverse effects Action ▪ nasal congestion ▪ peripheral inhibitor of dopa decarboxylase, ▪ (acromegaly, high dose) gastric haemor- rhage which normally decarboxylates levodopa to dopamine in the tissues, thereby pre- ▪ see general Adverse effects for dopamine agonists venting any therapeutic dose reaching the brain (levodopa but not dopamine can Interactions cross the blood–brain barrier). Bensera- zide prevents this peripheral decarboxyl- ▪ increased plasma levels may result if given with erythromycin ation from occurring so that the levodopa crosses the blood–brain barrier, before ▪ effects may be antagonised by phenothi- azines, butyrophenones, metoclopramide, conversion to dopamine, allowing substan- methyldopa, TCAs, pimozide, oestrogens tially lower doses of levodopa to be used and thyrotropin-releasing factor (e.g. benserazide and levodopa 200 mg is equal to 1000 mg levodopa alone) ▪ effects may be increased if given with levodopa or clonidine ▪ at therapeutic dose, does not cross the blood–brain barrier ▪ caution if given with azole antifungal agents or protease inhibitors Use ▪ see general Interactions for dopamine ago- ▪ given with levodopa in the treatment of Parkinson’s disease or parkinsonism nists Nursing points/Cautions Note ▪ it has yet to be established that the 10 mg ▪ combined with levodopa in Madopar prep- arations capsule is the bioequivalent of two 5 mg capsules or four 2.5 mg tablets ▪ advise patient to take initial doses at bed- time, to reduce the incidence of hypoten- BROMOCRIPTINE (Kripton, sion and loss of consciousness Parlodel) ▪ gastric irritation is reduced if bromocrip- tine is taken with or immediately after Available forms food Tablets: 2.5 mg; Capsules: 5 mg, 10 mg ▪ dosage increases are made gradually, start- ing with smallest dose, usually over several Action ▪ ergot derivative with no uterotonic and little vasoconstrictor activity ▪ days, to reduce adverse effects decreasing dose usually stops auditory/ ▪ stimulates dopaminergic receptors visual hallucinations ▪ inhibits release of prolactin 355
  • 9. HAVARD’S NURSING GUIDE TO DRUGS ▪ (Parkinson’s disease) may be given as Adverse effects mono or combination therapy ▪ leg oedema ▪ warn patient that alcohol may cause nau- ▪ dyspnoea sea, abdominal pain and bloating during ▪ see general Adverse effects for dopamine agonists bromocriptine therapy ▪ (long-term therapy) women should have Interactions ▪ regular gynaecological examinations patient should be advised to report any ▪ not recommended with other ergot alka- loids back pain or oedema of lower limbs imme- diately (signs of retroperitoneal fibrosis) ▪ not recommended with macrolide antibac- terial agents (e.g. erythromycin) ▪ (Parkinson’s disease) regular X-ray moni- toring is recommended to detect pulmo- ▪ see general Interactions for dopamine ago- nists nary fibrosis ▪ warn patients with acromegaly to immedi- Nursing points/Cautions ately report any GI side-effects ▪ administration with food may lessen GI ▪ tablets not recommended in those with disturbances galactase intolerance, severe lactase defi- ▪ see general Nursing points/ Cautions for dopamine agonists ciency or glucose/ galactose malabsorption ▪ see general Nursing points/Cautions for ▪ contraindicated in those with hypersensi- tivity to any ergot alkaloid dopamine agonists ▪ caution if used in those with suspected/ known peptic ulceration or diabetes not recommended during preg- nancy or breastfeeding (expec- ▪ contraindicated in those with sensitivity to ergot alkaloids, uncontrolled hyper- ted to inhibit lactation) tension, toxaemia, hypertensive disorders before starting therapy, preg- associated with pregnancy (including post- nancy should be excluded and partum), coronary artery disease, severe at least 1 month should elapse cardiovascular conditions or serious psy- between stopping treatment chiatric disorders and becoming pregnant CABERGOLINE (Cabaser, CARBIDOPA Dostinex) Action Available forms Tablets: 500 microgram,1 mg, 2 mg, 4 mg ▪ inhibits peripheral decarboxylation of levodopa increasing the amount that Action enters the brain for conversion to dopa- ▪ ergot derivative mine ▪ stimulates D2-dopamine receptors, inhibit- ▪ does not cross the blood–brain barrier in therapeutic doses ing prolactin secretion ▪ central dopaminergic effect Use Use ▪ given with levodopa to treat parkinsonism ▪ Parkinson’s disease (Cabaser only) Note ▪ inhibiting physiological lactation, hyperpro- lactinaemia (see Pregnancy, childbirth and ▪ combined with levodopa in Duodopo Intestinal Gel, Kinson, Levohexal, Sinemet breastfeeding) and Sinemet CR Dose ▪ combined with levodopa and entacapone ▪ (Parkinson’s disease, not previously treated) initially 0.5–1 mg orally daily, in Stalevo increasing at weekly intervals to 2–4 mg orally daily (monotherapy) or 2–6 mg orally daily (adjunct to levodopa) 356
  • 10. ANTI-PARKINSON’S AGENTS LEVODOPA Interactions ▪ effects enhanced by the peripheral dopa decarboxylase inhibitors, carbidopa and Available forms benserazide Capsules: levodopa 50 mg/benserazide 12.5 mg, levodopa 100 mg/benserazide 25 ▪ not recommended with baclofen or meto- clopramide mg, levodopa 200 mg/benserazide 50 mg; Capsules (sustained release): levodopa 100 ▪ contraindicated with or within 14 days of MAOIs mg/benserazide 25 mg; Tablets: levodopa 100 mg/benserazide 25 mg, levodopa 200 ▪ not recommended with halothane as com- bination may result in arrhythmia mg/benserazide 50 mg; Tablets (dispersible): levodopa 50 mg/benserazide 12.5 mg,levodopa ▪ not recommended with phenothiazines or butyrophenones (e.g. haloperidol) as 100 mg/benserazide 25 mg effects of levodopa may be reduced Tablets: levodopa 100 mg/carbidopa 25 mg, levodopa 250 mg/carbidopa 25 mg; Tablets ▪ bioavailability decreased if given with iron- containing products (sustained release): levodopa 200 mg/ carbidopa 50 mg; levodopa 50 mg/carbidopa ▪ effects may be reduced if given with anti- psychotic agents, papaverine or phenytoin 12.5 mg/entacapone 200 mg, levodopa 100 mg/carbidopa 25 mg/entacapone 200 ▪ risk of dyskinesia increased by prolonged therapy mg, levodopa 150 mg/carbidopa 37.5 mg/ entacapone 200 mg, levodopa 200 mg/ ▪ increased serum levels may occur if given with penicillamine or methyldopa carbidopa 50 mg/entacapone 200 mg ▪ action may be inhibited by opioids Intestinal gel (plastic cassette): levodopa 20 mg/carbidopa 5 mg/mL ▪ not recommended with adrenaline, nor- adrenaline, isoprenaline or dexamphet- Action amine as effects may be increased by ▪ immediate precursor of the synaptic neu- rotransmitter, dopamine levodopa Nursing points/Cautions ▪ decarboxylation occurs in peripheral tis- sues as well as the CNS, thereby decreas- ▪ should be taken 30–60 minutes before food if possible. However, gastric irritation ing the amount of levodopa entering the is reduced by taking with or immediately CNS to be converted to dopamine after food, if needed ▪ peripheral decarboxylation is inhibited by benserazide or carbidopa ▪ gastrointestinal and cardiovascular adverse effects may be decreased when given with Use peripheral decarboxylase inhibitor ▪ all types of parkinsonism, except drug- ▪ advise patient about the need to continue treatment because it is long-term replace- induced parkinsonian symptoms ▪ controls akinesia and rigidity more effec- tively than tremor ment therapy; maximum improvement may take up to 6 months and is maintained only while therapy continues Dose ▪ rarely used alone ▪ conduct monthly FBC and monitor hepatic, renal and cardiovascular function Adverse effects during prolonged therapy ▪ muscle cramps, hypotonia ▪ sudden fluctuations of effectiveness of ▪ cardiac arrhythmias, palpitations levodopa develop after about 2 years of ▪ dyskinesia, hyperkinesia, involuntary move- therapy (‘on–off’ effect) ments, bradykinetic episodes (‘on–off’ ▪ those with diabetes are advised to moni- tor blood glucose concentrations closely phenomenon), end of dose deterioration, freezing episodes during therapy ▪ dark urine ▪ advise patient to select the correct formu- ▪ (uncommon) haemolytic anaemia, tran- sient leucopenia lation and that they are not interchange- able ▪ see general Adverse effects for dopamine ▪ a reddish tinge in the urine is harmless; tears and sweat may also appear brown agonists 357
  • 11. HAVARD’S NURSING GUIDE TO DRUGS ▪ appearance of involuntary movements is a sign of levodopa toxicity stomach. Intestinal gel (cassette) should be stored at 2–8°C ▪ levodopa therapy is discontinued at least ▪ caution if used in those with epilepsy, depression, history of psychosis, cardiac 2–3 days before surgery and restarted as soon as the patient is able to take oral arrhythmias or myocardial infarction (ther- medications apy should be started as an inpatient), or his- ▪ (sustained release tablets/capsules) swal- low whole, do not chew or crush, however ▪ tory of peptic ulcer not recommended in those with a his- tablets can be divided without affecting tory of malignant melanoma or suspicious properties. Because the onset of action lesion because therapy may activate a of sustained release preparations is long, malignant melanoma patient may also need to take an immediate ▪ contraindicated in those with any hypersen- sitivity to sympathomimetic amines, if under release preparation for immediate effects ▪ dispersible tablets should be dissolved in 25–50 mL water (solution is milky white) 30 years of age, or with uncompensated car- diovascular, endocrine, kidney, liver or blood and drunk within 30 minutes. Ensure that disease, narrow-angle glaucoma, active psy- solution is well stirred chosis or psychoneurosis, intention tremor ▪ dispersible tablets are recommended for or Huntington’s chorea those with swallowing difficulties or if not recommended during preg- rapid onset of action is required nancy or breastfeeding ▪ (intestinal gel) gel is administered directly into the duodenum, initially via a tem- Note porary nasoduodenal tube to confirm ▪ may be used in combination with anticho- linergic agents positive clinical response (maximising functional ‘on’ time and minimising the ▪ combined with benserazide in Madopar preparations disabling ‘off’ periods) before the inser- tion of a permanent percutaneous endo- ▪ combined with carbidopa in Duodopa Intestinal Gel, Kinson, Levohexal, Sinemet scopic gastrostomy (PEG) tube (tube placement should be confirmed before and Sinemet CR administration). Gel is administered con- ▪ combined with carbidopa and entacapone in Stalevo tinuously using a portable pump (CADD- Legacy Duodopa (CE 0473)). Dosage consists of morning bolus dose (100–200 PERGOLIDE (Permax) mg), continuous maintenance dose (20–200 mg/hour) and extra boluses Available forms (given if patient becomes hypokinetic dur- Tablets: 50 microgram, 250 microgram, 1 mg ing the day, usually between 10 and 40 mg). If extra boluses are given more than Action 5 times per day, the continuous mainte- ▪ ergot derivative nance dose should be recalculated. The morning bolus dose may also require ▪ stimulates postsynaptic dopaminergic recep- tors in nigrostriatal system adjusting. The gel should only be admin- istered for a total of 16 hours, after ▪ dopamine agonist similar to but more potent than bromocriptine (see earlier), which the cassette should be discarded, with action on D1, D2 and D3 receptors regardless of whether any gel remains in ▪ inhibits prolactin secretion the cassette or not. If the administration continues over night, the cassette must ▪ transiently increases the concentration of growth hormone and decreases that of still be changed after it has been at room luteinising hormone temperature for 16 hours. Continuous administration may result in tolerance and ▪ active metabolites reduction of therapeutic effect. If a sudden Use deterioration in effect is seen, placement ▪ adjunctive treatment in Parkinson’s disease of the tube should be checked as it may Dose become displaced from duodenum into the ▪ initially 50 microgram orally daily for 2 days, then increasing by 100–150 microgram/day 358
  • 12. ANTI-PARKINSON’S AGENTS every 3rd day for 12 days, with further Adverse effects increases of 250 microgram/day every ▪ cough, dyspnoea, nasal congestion 3rd day until a therapeutic response is ▪ flushing achieved (usually given in 3 divided doses) (maximum daily dose 5 mg) ▪ back pain, pain in extremities, arthralgia, muscle cramps, myalgia Adverse effects ▪ (rare) rhabdomyolysis ▪ rhinitis, dyspnoea ▪ see general Adverse effects for dopamine ▪ double vision agonists ▪ tachycardia, palpitations Interactions ▪ abnormal liver function ▪ when given with levodopa, dose of ▪ see general Adverse effects for dopamine levodopa should be reduced agonists ▪ serum levels may be increased by cimetidine, digoxin, diltiazem, quinine, Interactions ▪ see general Interactions for dopamine ago- nists ranitidine, triamterene, trimethoprim and verapamil Nursing points/Cautions ▪ may increase serum levels of cimetidine, digoxin, diltiazem, quinine, ranitidine, triam- ▪ patient should be carefully monitored for terene, trimethoprim and verapamil any signs of confusion or hallucinations because this may require cessation of ther- ▪ see general Interactions for dopamine ago- nists apy Nursing points/Cautions ▪ see general Nursing points/Cautions for dopamine agonists ▪ see general Nursing points/Cautions for ▪ caution if given to those with cardiac arrhythmias dopamine agonists ▪ contraindicated in those with hypersensi- tivity to ergot derivatives ROTIGOTINE (Neupro) Available forms PRAMIPEXOLE (Sifrol) Transdermal patches: 2 mg/24 hour, 4 mg/24 hour, 6 mg/24 hour, 8 mg/24 hour Available forms Action Tablets: 125 microgram, 250 microgram, 1 g ▪ activates D1, D2 and D3 receptors in the brain Action ▪ dopamine agonist that binds selectively to ▪ also has 5HT1D receptor and alpha1A-adre- noceptor activity dopamine D2 and D3 receptors Use Use ▪ Parkinson’s disease (alone or with ▪ Parkinson’s disease (alone or with levodopa) levodopa) Dose ▪ restless leg syndrome ▪ (early stage Parkinson’s disease) initially Dose 2 mg/24 hour patch applied daily, then ▪ (Parkinson’s disease) initially 125 micro- gram orally 3 times daily, increasing to 250 increased at weekly intervals of 2 mg/24 hour to an effective dose (maximum 8 mg/ microgram orally 3 times daily after 5–7 24 hours) OR days, then to 500 microgram orally 3 times ▪ (advanced stage Parkinson’s disease) ini- tially 4 mg/24 hour patch applied daily, then daily after a further 5–7 days, with further increases at weekly intervals if needed increased at weekly intervals of 2 mg/24 (daily maximum 4.5 mg) OR hour to an effective dose (maximum 16 ▪ (restless leg syndrome) initially 125 micro- gram orally daily 2–3 hours before bed- mg/24 hours). For doses above 8 mg/24 hours, combination of patches can be used time, increasing every 4–7 days to 750 Adverse effects microgram daily if needed ▪ increased liver enzymes 359
  • 13. HAVARD’S NURSING GUIDE TO DRUGS ▪ (application site) erythema, pruritus, irri- tation, burning, dermatitis, vesicle, blister, ▪ patients should be advised to report any application site reaction that either pain, hypersensitivity spreads beyond the site or persists for ▪ see general Adverse effects for dopamine more than 2–3 days agonists ▪ direct sunlight should be avoided to any application site rash or irritation until the Interactions skin heals ▪ see general Interactions for dopamine ago- nists ▪ patients should be advised to avoid exter- nal heat (e.g. excessive sunlight, heating Nursing points/Cautions pads, sauna, hot bath) to the transdermal ▪ patients should be advised to apply patch patch area at approximately the same time each day and to leave in situ for 24 hours ▪ patients should be instructed in the cor- rect disposal of the transdermal patch ▪ transdermal patch should be applied to clean, dry, intact skin on upper arms, shoul- (i.e. folded in half without matrix exposed, placed in original sachet and discarded out ders, hip, flank, thigh or abdomen of the reach of children) as it still contains ▪ transdermal patch can be left intact when active substance swimming or bathing ▪ see general Nursing points/ Cautions for ▪ transdermal patch should not be cut into dopamine agonists smaller pieces ▪ contraindicated with cardioversion or ▪ patients should be advised to rotate applica- tion sites daily and not use the same site magnetic resonance imaging (MRI) due to the risk of skin burning because of the alu- within 14 days minium backing layer MONOAMINE OXIDASE TYPE B ENZYME (MAO-B) INHIBITORS SELEGILINE (Eldepryl, Selgene) ▪ dizziness, vertigo, insomnia, sleep disorders, headache, fatigue Available forms ▪ dyskinesia Tablets: 5 mg ▪ dyspnoea Action ▪ rash ▪ selectively inhibits MAO-B enzyme (breaks ▪ difficulty with micturition down dopamine in the brain), thereby ▪ anxiety, confusion, hallucinations, agitation, depression increasing the concentration of dopamine ▪ active metabolites ▪ increase in liver enzymes (ALT, AST) ▪ elimination half-life is approximately 1–2 Interactions hours ▪ severe hypotension may result if given with non-selective MAOIs Use ▪ as an adjunct to levodopa therapy in ▪ increased tyramine sensitivity may result if given with moclobemide. If given together, patients with late-stage Parkinson’s disease a low-tyramine diet is recommended (see or monotherapy in early disease Cheese reaction in Glossary for a list of Dose foods to avoid) ▪ 5 mg orally twice daily with breakfast and ▪ pethidine is contraindicated with or within 14 days of stopping selegiline lunch Adverse effects ▪ contraindicated with SSRIs. Selegiline should be stopped for 2 weeks before ▪ anorexia, nausea, vomiting, abdominal pain, constipation, dry mouth, hiccups starting SSRIs or SSRIs should be stopped for 5 weeks before starting selegiline ▪ postural hypotension, syncope, palpita- tions, oedema ▪ caution if given with tramadol ▪ angina, arrhythmias ▪ hypertension may occur if given with dopa- mine 360
  • 14. ANTI-PARKINSON’S AGENTS ▪ increased bioavailability may occur if given with oral contraceptives containing ges- ▪ check supine and standing BP regularly for postural hypotension todene/ ethinyloestradiol or levonorg- estrel/ ethinyloestradiol ▪ advise patient to avoid postural hypoten- sion by moving gradually to a sitting or ▪ increased risk of serotonin syndrome (see standing position, especially after sleep Glossary) if given with SSRIs,TCAs, clozap- ine or ecstasy (3,4-methylenedioxy-meth- ▪ advise patient to resume physical activity gradually to avoid injury amphetamine) ▪ patient should be advised to avoid driving ▪ may increase adverse effects of levodopa or operating machinery if dizziness, vertigo, ▪ increased risk of CNS toxicity if given with fatigue or hypotension occurs TCAs, therefore these should be stopped 2 weeks before starting selegiline ▪ caution if used in those with peptic/ duo- denal ulcers, labile hypertension, arrhyth- mia, severe angina or psychosis as these Nursing points/Cautions conditions may be exacerbated ▪ dose of levodopa can be reduced by 10–30% after 2–3 days if levodopa-related ▪ caution if used in those with severe kidney or liver dysfunction adverse effects occur ▪ patient should be carefully monitored for not recommended during preg- any signs of confusion or hallucinations nancy or breastfeeding unless because this may require cessation of ther- benefits outweigh the risks apy ▪ patient should bebecause it not to stop therapy suddenly warned may precipi- tate hallucinations and confusion 361

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