Drugs #4

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MAO-Is

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Phenylzine, tranylcypromineMOA – Irreversibly inhibit monoamine oxidase A and B increasing synaptic concentrations of adrenaline, noradrenaline, dopamine and serotoninIndications – Second line in major depression and some anxiety disordersPrecautions – Contraindicated with triptans (ischaemia), in angina (rebound tachycardia exacerbates), lower the seizure threshold, bipolar, drugs that contribute to serotonin toxicityDrugs that are contraindicated within 14 days of a MOA-IDexamethasone, dextromethorphan, entacapone, fentanyl, pseudoephedrine, tramadol, phentermine and all antidepressantsAvoid use in significant hepatic diseaseSEs – Orthostatic hypotension, sleep disturbance, headache, fatigue, constipation, weight gain, twitching, tremors, rare hypertensive crisisTake before 3pm, avoid tyramine foods for 2 weeks afterTell your doctor if you develop frequent headaches and stop taking immediately if you experience tremors or severe headache

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SSRIs

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Fluoxetine, sertraline, paroxetine, vortioxetine, citalopram, escitalopram, fluovoxamineMOA – Inhibit presynaptic uptake of serotoninIndications – Major depression, anxiety disorders (not citalopram), bulimia (fluoxetine) and premenstrual dysphoric disorder(sertraline)Precautions – Lower seizure threshold, bipolar, patients at risk of bleeding, risk factors for close-angle glaucoma, drugs that may cause hyponatraemia, serotonin toxicity, dose reduce in hepatic impairment, renal for paroxetineSEs – Nausea, diarrhoea, agitation, insomnia, drowsiness, sexual dysfunction, weight gain or loss, dizziness, headache, increased suicidality (particularly in young people)Citalopram and escitalopram – May increase QTFluoxetine – Long half-life of 16 days – Less withdrawal effects but SEs may persistDon’t drive until you know how it affects you, L9, L5, take fluvoxamine/paroxetine with foodDoses for OCD or eating disorders is usually higher and lower for other anxiety disordersReduce the daily dose by half no greater than weekly

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TCAs

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Amitriptyline, clomipramine, dothiepin, doxepin, imipramine, nortriptyline, trimipramineMOA – Inhibit uptake of NA and 5HT into presynaptic terminalsIndications – Major depressionAmitriptyline – Nocturnal enuresis, adjuvant in pain management, migraine prophylaxisPrecautions – Risk factors for close-angle glaucoma, lowers the seizure threshold, hyperthyroidism may have enhanced response to TCAs, significant adverse effects with ischaemic heart disease and CHD, QT prolongation, high risk with overdose, bipolar, serotonin toxicity, dose reduce in hepatic, lower doses in the elderly, Cat CSide Effects – Sedation, dry mouth, constipation, dizziness, urinary retention, blurred vision, weight gain, sexual dysfunctionMay increase the effects of alcohol, L9, avoid driving until you know how it affects youDose for depression in all is 75-150mg, usually max 300mg (150mg for nortrip)

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SNRIs

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Desvenlafaxine, venlafaxine, duloxetineMOA – Inhibit serotonin and NA reuptakeIndications – Major depression, Duloxetine = Anxiety and painful diabetic neuropathy, anxiety disorders for venlafaxinePrecautions – Bipolar, serotonin toxicity, lowers seizure threshold, risk factors for close-angle glaucoma, high risk of bleeding, treatment with drugs that cause hyponatraemia, dose reduce in renal impairment, duloxetine is contraindicated in hepatic impairment and dose reduce venlafaxineSide Effects – Nausea, dry mouth, constipation, yawning, sweating, sexual dysfunction, insomnia, blurred vision, headache, hypertensionDon’t drive until you know how it affects you, L9Take duloxetine and venlafaxine with food, duloxetine is the most likely antidepressant to be ceased by patients because of nausea and insomnia

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Agomelatine

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Valdoxan MOA – Unclear – Affects melatonin and serotonin receptorsIndications – Major depressionPrecautions – Bipolar, excessive use of alcohol may increase risk of hepatotoxicity, contraindicated in hepatic impairment, serotonin toxicitySEs – Increased aminotransferases, dizziness, abdo painDose – 25-50mg at bedtimeDon’t drive until you know how it affects you, L9

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Tetracyclics

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Mianserin (Lumin) and mirtazapineMOA – Increases central noradrenergic transmission by blocking alpha2-adrenergic receptorsMirtazapine also blocks 5HTIndications – Major depressionPrecautions – Serotonin toxicity, lowers seizure threshold, bipolar, risk factors for prolonged QT, dose reduce in renal and hepatic impairment (mianserin)SEs – Mianserin - Sedation, dry mouth, dizziness, vertigoMirtazapine – Weight gain, sedation, weakness, peripheral oedemaDon’t drive until you know how it affects you, L9

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Moclobemide

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MOA – MOA-A inhibitor – Synaptic concentrations of serotonin, noradrenaline and dopamine are increasedIndications – Major depression, anxiety disordersPrecautions – Serotonin syndrome, bipolar, dose reduce in hepatic impairmentSEs – Nausea, dry mouth, constipation, anxiety, restlessness, insomnia, headacheDose – 300-600mg in the morning with food

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Reboxetine

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MOA – Inhibits NA reuptake and weakly 5HTIndications – Major depressionsPrecautions – Serotonin syndrome, bipolar, lowers seizure threshold, risk factors for close-angle glaucoma, cardiovascular disease, dose reduce in renal and hepatic impairmentSEs – Urinary retention, dysuria, urinary frequency, dry mouth, nausea, constipation, orthostatic hypotension, increased diastolic BP, tachycardiaDose 4-6mg BDDon’t drive until you know how it affects you, L9

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Buprenorphine

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Subutex and suboxone (inc. naltrexone)MOA – Partial agonist – Reduces withdrawal and craving for opioidsIndications – Maintenance of opioid dependence and opioid withdrawalPrecautions – Contraindicated in severe respiratory insufficiency, contraindicated if intoxicatedUse low doses and review frequently for patients using benzos and alcoholContraindicated in hepatic impairmentSEs – Constipation, dyspepsia, hypotension, nausea and vomitingTakes 2-10 minutes for the tab to dissolveFirst dose = Precipitated withdrawalSuboxone – Naltrexone is included to discourage diversion, little use SL but if injected it will antagonise other opiates

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Varencicline

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MOA – Partial agonist at nicotinic acetylcholine receptorsIndications – Nicotine dependencePrecautions – Psychiatric conditions may worsen, use cautiously with a history of seizures, use with NRT increases side effects, dose reduce in renal impairmentSEs – Nausea, sleep disturbance, vivid dreams, dizziness, headache, weight gainReports of suicidal ideationDose – 0.5mg initially then up to 1mg BD

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Naltrexone

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MOA – Opioid antagonist – Reduces cravings for alcohol and possibly reduces some of the pleasurable side effectsIndications – Alcohol dependence and adjunct in maintenance of abstinence from opioids after detoxificationPrecautions – Contraindicated in acute withdrawal and patients being treated with opioids for painContraindicated in acute hepatitisSEs – Nausea, headache, dizziness, anxiety, fatigue, insomnia – Usually subside within two weeksRare hepatotoxicity – Monitor for jaundice, frequent LFTsDose – 50mg dGreat risk of fatal overdose if you stop taking naltrexone and use opioids again

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Acamprosate

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MOA – Unclear – Possibly involves restoration of normal activity in glutamate and GABA-ergic systems – Reduce cravings, increase alcohol-free days and reduce alcohol intake during relapseIndications – Maintenance of abstinence in alcohol dependencePrecautions – Contraindicated in renal impairmentSEs – Rash, diarrhoea, abdo pain, itch, erythemaDose – 2 tabs tds or 2 in the morning and one at lunch and dinner (if <60kg)

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Z Drugs

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Zopiclone, zolpidemMOA – Potentiate the inhibitory effects of GABAIndications – Short term management of insomniaPrecautions – Acute or severe pulmonary insufficiency (zolpidem), contraindicated with alcohol as it increases the risk of dangerous behaviourMay worsen depression, psychosis and schizophreniaUse low doses in hepatic impairment and the elderlySEs – Diarrhoea (zolpidem), bitter taste and dry mouth with zopiclone, impaired alertness the next dayInfrequent – Risky behaviour e.g. sleep walking, sleep driving e.t.cDose – Zolpidem – 5mg IR or 6.25mg CRZopiclone – 3.75-7.5mgAvoid driving the next day until you know how you’re affectedDo not take alcohol or other medications that may cause drowsinessReports of dependence, tolerance and misuse

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Benzodiazepines

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MOA – Potentiate the inhibitory effects of GABA resulting in anxiolytic, sedative, hypnotic, muscle relaxant and ant-epileptic effectsIndications – Anxiety, insomnia (clobazam, temazepam, flunitrazepam, lorazepam, nitrazepam, oxazepam, triazolam), seizures (clobazam)Diazepam – Muscle relaxant, acute alcohol withdrawal, conscious sedationPrecautions – Contraindicated in respiratory depression, increased sensitivity to CNS effects in renal impairment, contraindicated in severe hepatic impairmentSEs – Drowsiness, light-headedness, memory loss, hypersalivation, slurred speech, ataxiaAvoid alcohol, if you take it for more than 2-4 weeks tolerance and dependence may develop and withdrawal symptoms may appear upon cessation

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Antipsychotics

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Amisulpride, aripiprazole, asenapine, chlorpromazine, clozapine, droperidol, flupenthixol (inj), fluphenazine (inj), haloperidol, Olanzapine, pericyazine, quetiapine, risperidone, trifluoperazine, ziprasidone, zuclopenthixolMOA – Thought to be due, at least in part, to dopamine blockade in various parts of the brainIndications – Acute and chronic psychosis, bipolarPrecautions – Aggrevate Parkinson’s, lower seizure threshold , increased risk of dystonia with hyperthyroidism, QT prolongation, close-angle glaucoma, diabetes – increased BGLs, caution with hepatic impairment, increased risk of stroke and death in the elderlySEs – Sedation, anxiety, agitation, EPSE, weight gain, increased BGLs, constipation, dry mouth, sexual adverse effects and orthostatic hypotensionClozapine, olanzapine and quetiapine – Increased BGLs, dislipidaemia and weight gainChlorpromazine – Skin reactions due to light exposureRare life threatening neuroleptic malignant syndrome – Fever, muscle rigidity, altered consciousness – Can occur anytime during treatment, more common in young menStopping treatment is associated with a high risk of relapse and suicideDon’t drive until you know how it affects you, increases the effects of alcohol, L9 to avoid relapse and withdrawal symptoms (tachycardia, sweating, insomnia)Routine full blood counts and LFTs are advisable – Mandatory for clozapineSmoking – Increases clearance of clozapine, caffeine affects it tooOlanzapine, paliperidone, risperidone, zuclopenthixol– Long acting injection

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Lithium

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MOA – Unknown – Inhibition of dopamine release, enhancement of serotonin release and decreased formation of intracellular second messengers. Little or no effect in normal individualsIndications – Prevention of manic episodes in bipolar, treatment of acute mania, schizoaffective disorder and chronic schizophreniaPrecautions – Hyponatraemia increases risk of lithium toxicity, treat hypothyroidism before starting lithium, psoriasis may be exacerbated, serotonin toxicity, caution in elderly – more susceptible to SEs and poor renal functionReduce dose even in relatively mild renal impairmentCat D – Congenital heart defectsSEs – Metallic taste, nausea, diarrhoea, epigastric discomfort, weight gain, fatigue, vertigo, hypothyroidismSigns of toxicity – Thirst, blurred vision, increasing diarrhoea, nausea, drowsiness, muscle weakness, flu-like illness. Severe = Movement disturbances, coma, seizuresConcentration monitoring – Every three months - More frequent during illness, pregnancy e.t.cCheck serum calcium, thyroid levels and renal function every 3-6 months, consider EEG for cardiovascular diseaseTake with food, maintain a normal diet and fluid intake, drink more during hot weatherL9 – To avoid relapseAvoid sodium bicarbonate – Antacids, Ural – Makes lithium less effective