Here are the Neuropharmacology reference notes. There are many resources devoted to this online and offline. This section is used as a quick study reference or as a starting point for further study. Hope you find it useful!
 

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Please see disclaimer for details. None of this information is medical advice or endorsement for practicing medicine a certain way. These are merely a study aid. This list was started offline in 2003 and has been updated intermittently since then.  It is still useful as a study aid so it is included here.
Please note that this section does not constitute a formulary or imply any prescribing information. The dosing information is for educational purposes only, please consult your physician and official prescribing information.

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Name	Mechanism of Action	Dosing & route	Indication	Side effects & contraindications	Comments, monitoring etc
Phenobarbital * (Phenobarbitone)	GABAA enhancer increases duration of Cl- channel opening		1. Generalised & parital epilepsy, 2. no longer frontline agent 3. induction of anaesthesia & in Criglar-Najjar syndrome type 2 to induce the expression of glucuronyl transferase	induces CYP 2C9 Contraindication: porphyria. also
Valproate * valproic acidosis, sodium valproate				Pregnancy category X. Side effects: teratogenic, hepatotoxic (mitochondrial), hyponatremia, rash, tremor, ataxia. Contraindication: liver disease	Monitor Liver enzymes & ammonia NH4
Phenytoin			used for status epilepticus	*Side effects: teratogenic, gingival hyperplasia, hypertrichosis, nystagmus & diplopia, vitamin D deficiency, hepatotoxic (immunologic). Contraindication: sinus bradycardia, heart block	Monitor ECG +BP if intravenous
Carbamazepine *				Side effects: diplopia/nystagmus, leucopenia, aplastic anemia, hepatitis, generalised rash, anti-cholinergic, SIADH, teratogenic. Contrainidation: if HLA-B*1502 then high risk for Stevens Johnson syndrome and toxic epidermal necrolysis. CYP1A2, CYP3A4 inducer.	Monitor FBC.
Ethosuximide *	Ca++ channel blocker T-type:		1st line in absence seizures only	Side effect: Stevens-Johnson syndrome
Benzodiazepines (entire class):	GABAA enhancer (increases frequency)		1. Status epilepticus: lorazepam. 2. Cluster of seizures: lorazpeam, diazepam, clonazepam	Side effects: decreases REM sleep, sedation, dependence, impaired memory & amnesic disorder
Lorazepam*
Diazepam * status epilepticus (Valium-trade name)			REM sleep behaviour disorder: clonazepam	Side effects: withdrawal (anxiety, seizures, insomnia, abnormal experiences)
Clonazepam used for absence & myoclonus
Lamotrigine *	blocks Na+ channel, also decreases glutamate & aspartate release			Side effects: Stevens-Johnson syndrome
Vigabatrin	GABA transaminase inhibitor
Gabapentin			partial & tonic-clonic, also for neuropathic pain
Topiramate	Na+ blocker, GABA agonist, decreases glutamate activity		Adjunct in partial seizures. migraine prophylaxis.	Side effects: mental dullness, kidney stones, paraesthesia that resolves, weight loss, metabolic acidosis, visual impairment. Contraindication: pregnancy, breast feeding.	monitor U&E after 2 weeks
Levetiracetam	binds to synaptic vesicle protein SVA2
Zonisamide				Side effects: metabolic acidosis	Monitor serum bicarbonate
Oxcarbazepine
Clobazam
Tiagabine				Side effects: seizures in nonepileptics
Magnesium sulfate (MgSO4, sulphate	interacts with NMDA receptor, given to women with preeclampsia at labour & women with eclampsia	intravenous i.m. (if given oral it’s a laxative)	Used in Eclampsia	Side effects: loss of tendon reflexes, confusion, coma, respiratory depression.	Calcium gluconate is the antidote. Monitor reflexes, respiratory rate & urine output.
Perampanel	selective alpha-amino-3-hydroxy-5-methyl-4-isoxazolprepionic acid (AMPA) receptor antagonist

 

Cerebrovascular medications:

 

Name	Mechanism of Action	Dosing & route	Indication	Side effects & contraindications	Comments, monitoring etc
Thrombolytic drugs: (plasminogen activators):
Alteplase * a.k.a. Tissue plasminogen agent (tPA)	activates plasminogen that is bound to fibrin	Intravenous	Ischemic stroke within 4.5 hrs of symptom onset
Antiplatelets
Aspirin	Irreversible COX inhibitor: (inhibits TXA2 synthesis)	Oral, rectal	Ischemic stroke
Clopidogrel	P2y12 inhibitor, non-competitive, ADP receptor antagonists, Decrease platelet activation	Oral	Ischemic stroke
Ticlopidine	P2y12 inhibitor, non-competitive, ADP receptor antagonists, Decrease platelet activation
Dipyridamole	Platelet PDE inhibitor raising cAMP	Oral	Ischemic stroke	GI effects, hypotension & tachycardia, hot flushes, worsening symptoms of coronary heart disease, dizziness, myalgia, throbbing headache, hypersensitivity, bleeding; rarely thrombocytopenia. Contraindications: Recent MI, angina, hypotension, myasthenia gravis	add on to aspirin in stroke)
Cilostazole		Oral	Ischemic stroke
Non-K Oral Anti-Coagulants NOAC:
Apixaban	Factor Xa inhibitor anticoagulant	Oral, BID	Atrial fibrillation	Contraindication: hepatic disease with coagulopathy,	Metabolised by CYP3A4 and P-glycoprotein (P-gp). Lower dose in patients with at least 2 of the following characteristics: age >80 years, body weight <60 kg, or serum creatinine <1.5 mg/dL. Test levels by anti-Xa assays.
Dabigatran	Direct thrombin inhibitor	Oral, BID	Atrial fibrillation, DVT/PE	Gastritis, GI bleeding	P-gp,
Rivaroxaban	Factor Xa inhibitor	Oral, once or twice daily	Atrial fibrillation, DVT/PE	Contraindication: severe renal impairment,	CYP3A4, test levels by rivaroxaban sensitive PT assays, or anti-Factor Xa chromogenic assays using validated calibrators and controls
Edoxaban	Factor Xa inhibitor i	Oral, once daily	Atrial fibrillation, DVT/PE	Bleeding, abnormal LFTs, Contraindication: renal failure, also contraindicated in high creatinine clearance > 95 ML/MIN,	Test levels by anti-Xa assays.
Anticoagulants:
Warfarin	Inhibit epoxide reductase–> inhibit reduction of oxidised vitamin K–> blocking g-carboxylation of factors II, VII, IX & X.–> increases PT. Also inhibit protein C & S–> procoagulant initially.	Oral	Atrial fibrillation	teratogenic. if overdose–> Phytomenadione (vitamin K1).	must monitor PT, INR.
Heparin		Intravenous, subcutaneous	Deep venous thrombosis
Enoxaparin	Increases potency antithrombin III, thus inhibiting factor II & X, –> increases APTT. Don’t cross the placenta–> safe in pregnancy. More specific for Xa.	Subcutaneous	Deep venous thrombosis	Don’t need to monitor APTT

 

Migraine medications:

 

Name	Mechanism of Action	Dosing & route	Indication	Side effects & contraindications	Comments, monitoring etc
Migraine Abortive
Migraine Abortive Treatment: 5HT1D receptor agonist. Drug interaction SSRI causes serotonin syndrome
Sumatriptan * also used for cluster headaches !chest discomfort Contraindication: coronary artery disease or prinzmetal’s angina	5HT1D receptor agonist
Zolmitriptan	5HT1D receptor agonist
Ergotamine partial agonist	5HT1D receptor partial agonist
Migraine Prophylaxis:
Amitriptyline	Tricyclic antidepressant
Pizotifen	5HT & histamine antagonist			weight gain
Cyproheptadine	5HT2 & histamine antagonist,		is also sometimes used in anorexia nervosa.
Propranolol	b-blocker
Flunarizine	Ca++ channel blocker

 

Multiple sclerosis medications:

 

Name	Mechanism of Action	Dosing & route	Indication	Side effects & contraindications	Comments, monitoring etc
Glatiramer acetate (copaxone) a.k.a. copolymer-1		s.c. daily
Interferon beta IFNb:
IFN beta 1a		s.c. i.m.		neutralising antibodies	Monitor LFTs
IFN beta 1b		s.c.		neutralising antibodies	Monitor LFTs
Mitoxantrone hydrochloride	Cytotoxic	intravenous infusion		Cardiomyopathy	Not used anymore. Monitor FBC, LFTs. Echocardiogram
Oral agents
Dimethyl fumarate (trade name is Tecfidera)	Unknown mechanism of action in multiple sclerosis. Activates the Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway. Also a nicotinic acid receptor agonist.	Oral (with food), BID	RRMS	Nausea, diarrhea, abdominal pain, flushing. <1% develop lymphopenia <0.5x10e9/L. Rarely angioedema, anaphylaxis. Very rarely PML. Transient eosinophilia. Uncommonly raised LFTs but usually <3 times normal	CBC with lymphocyte count at baseline, repeat <6 months, and then every 6-12 months to monitor for lymphopenia. Discontinue if lymphocyte count is < 0.5X10e9/L for 6 months. Aspirin 325mg 30min before oral dose my reduce flushing
Teriflunomide (trade name is Aubagio)	Impairs de novo pyrimidine synthesis. Reversible inhibitor of mitochondrial dihydroorotate dehydrogenase. Decreases circulating lymphocytes, active metabolite of Leflunomide	Oral, once daily	RRMS	Nausea, diarrhea, alopecia (hair thinning), elevated ALT. Contraindication: liver disease, pregnancy, trying to concieve, can be found in semen, live vaccinations.	LFTs and Bilirubin at baseline, then monthly for 6 months, then every 6 months thereafter. Bring up to date with immunizations prior to treatment.
Fingolimod (Gilenya)	A sphingosine 1-phosphate receptor modulator	Oral	RRMS, Aggressive Multiple sclerosis	Headache, liver transaminase elevation, diarrhea, cough, influenza, sinusitis, back pain, abdominal pain, and pain in extremity. Macular edema. Contraindications: Mobitz Type II 2nd degree or 3rd degree AV block or sick sinus syndrome, prolonged QTc =or>500msec, Class Ia OR Class III anti-arrhythmic drugs	Observe for bradycardia at initial dosing, ECG before therapy and 6 hours after first dose. Fundoscopic exam before and 3-4 months after starting therapy. LFTs at baseline and as required. Monitor PFTs as required. Monitor BP during treatment. Contraception during treatment and 2 months afterwards.
IV infusions (high efficacy agents):
Natalizumab	alpha 4 integrin antagonist, antibody against alpha 4 integrin,	Intravenous infusion		increases risk of Progressive multifocal leukoencephalopathy especially if in combination therapy, Liver failure, hypersensitivity reactions, antibodies against natalizumab.	Used as single agent. Monitor LFTs
Alemtuzumab	CD52-directed cytolytic monoclonal antibody	Intravenous infusion. Initial dose then another 1 year later	RRMS, aggressive multiple sclerosis (failing 2 other medications)	Serious autoimmune: ITP, anti-GBM disease. Malignancy: thyroid cancer, melanoma, lymphoproliferative disorders. Infusion reactions: anaphylaxis. Common: UTI, upper respiratory tract infection, pharyngitis, herpes virus infection, flushing, nausea, vomiting, abdominal pain, headache, rash. Contraindication: active infection, HIV. Contraindication: live virus vaccines during treatment.	Monitor: CBC with differential, creatinine, urinalysis at monthly for 48 months after last dose. TFTs at baseline and every 3months until 48 months after last infusion. Baseline and yearly skin examinations. Monitor for 2 hours after infusion for reactions. Corticosteroid premedication with dosages. Antivirals for herpes viruses starting with first dose and continuing for 2 months or until CD4+ lymphocytes recover to >200 cells per microliter (which ever occurs later). Restricted use through: Risk Evaluation Mitigation Strategy (REMS) Program.

 

Dementia medications:

 

Name	Mechanism of Action	Dosing & route	Indication	Side effects & contraindications	Comments, monitoring etc
Reversible Acetylcholinesterase inhibitors: whole class	Reversible Acetylcholinesterase inhibitors. Slow disease progression.		Alzheimer’s disease	nausea, abdominal pain	used for mild to moderate dementia
Rivastigmine
Galantamine					CYP 2D6, 3A4
Donepezil					CYP 2D6, 3A4
Tacrine				hepatotoxic
Other agents:
Memantine	NMDA receptor antagonist: slow disease progression used for moderate to severe dementia. Via inhibiting glutaminergic excitotoxicity or effects on hippocampal neurons

 

Parkinson’s disease and antiparkinsonian medications:

 

Name	Mechanism of Action	Dosing & route	Indication	Side effects & contraindications	Comments, monitoring etc
Precursor:
Levodopa * a.k.a. L-dopa always combined with Carbidopa (or benserazide) the combination is a.k.a. co-careldopa	Dopamine agonist	Oral	Parkinson’s disease	Side effects: increases dopamine–> vomiting, tachycardia, arrhythmia, hypotension, hallucintations, dyskinesia, insomnia, mydriasis, increases melanin–> brown saliva & urine. Postural hypotension, dystonia	Need to decrease the dose slowly to avoid akinesia
Consider adding catecholamine o methyl transferase COMT inhibitor:
Tolcapone	catecholamine o methyl transferase COMT inhibitor. Inhibits L-DOPA & dopamine breakdown in the periphery	Oral			Reduces ‘on’ & ‘off’ phenomenon
Entacapone	catecholamine o methyl transferase COMT inhibitor. Inhibits L-DOPA & dopamine breakdown in the periphery	Oral			Reduces ‘on’ & ‘off’ phenomenon
Dopamine recpetor agonists:			1st line for Parkinson’s disease or to control on-off effect. Also for microprolactinoma, because dopamine acting on D2 is a prolactin inhibitory factor		Increase & decrease dose slowly
Non-ergot Dopamine agonists–> no peripheral vasospasm
Pramipixole	D3 agonist
Ropinirole	D2 agonist
Erogot derived Dopamine receptor agonists: all are D2 agonists
Bromocriptine *				Side effects: vasoconstriction–> complicates peripheral vascular disease, pleural pericardial or retroperitoneal fibrosis–> check ESR first. hallucinations, orthostatic hypotension,
Carbegoline, Lisuride, Pergolide
If intravenous treatment is necessary:
Apomorphine +domperidone as it causes significant vomiting
Monoamine oxidase MAO-B inhibitors: allows decreases dopamine dose
Selegiline * a.k.a. deprenyl	irreversible MAO-B inhibitor
Rasagiline *	reversible MAO-B inhibitor
Increase dopamine release:
Amantadine					withdraw gradually
mACh antagonists: treatment for drug induced Parkinsonism
Benzatropine			Drug induced parkinsonism

 

Antipsychotics:

 

Name	Mechanism of Action	Dosing & route	Indication	Side effects & contraindications	Comments, monitoring etc
Antipsychotics, whole class: A.k.a. neuroleptics, formerly (major tranquillisers)	Therapeutic effect via D2 antagonism & possibly serotonin antagonism.		Psychosis	extrapyramidal (pseudoparkinsonism, akinesia, dystonia) tardive dyskinesia (abnormal writhering movements), akathesia (restless leg syndrome), neuroleptic malignant syndrome. D2 on pituitary–> prolactinemia–> Galactorrhoea, gynaecomastia, impotence. Treat parkinsonism & akathisia with anticholinergic e.g. benzatropine. Treat tarditive dyskinesia by switching to a low potency or atypical agent. neuroleptic malignant syndrome (hyperpyrexia +autonomic instablility + muscle rigidity)–> treat with dantrolene & dopamine agonist.
First generation (typical):
Low potency agents:
Chlorpromazine	CPZ D1-5, M, Alpha 1,H1 antagonism,		also used for intractable hiccups	esp. hepatitis, pigmentary eye deposits. Contraindications: in patient with seizure predisposition
Droperidol			used +fentanyl for analgesia a.k.a. neuroleptanaesthesia
Thioridazine				esp. cardiovascular, pigmentory retinopathy.	withdrawn for the market. Used under specialist supervision only
High potency agents:
Haloperidol	depot D2-4 antagonism	Oral, Intramuscular, intravenous
Prochlorperazine			Also an antiemetic
Pimozide				QT prolongation
Fluphenazine		Oral, Depot
Others (for reference):
Perphenazine, trifluoperazine
flupentixol (flupenthixol) depot, zuclopenthixol depot, pipotiazine depot, sulpiride, levomepromazine, pericyazine, benperidol
Second generation (atypical):	Act via serotonin antagonism (5HT2 & D4 antagonist), prefrontal cortex has the highest D4 concentration, useful for positive & negative symptoms			Decreases seizure threshold, but less of the other neurological effects, subjective dysphoria, drooling, some–> Q-T prolongation which may–> ventricular arrhythmia	Withdraw gradually
Risperidone	alpha 2 antagonism 1st line	Oral, Depot		1st dose hypotension–> titrate slowly, orthostatic hypotension, osteoporosis, sexual dysfunction, oesophageal dysmotility & aspiration, hyperprolactinemia, extrapyramidal effects at high doses
Olanzapine		Oral, Intramuscular	Also used in OCD	weight gain, hyperglycemia CI. angle closure glaucoma	effective against negative symptoms, some antidepressive effects
Quetiapine		Oral		cataracts. Second least likely to cause extrapyramidal symptoms
Zisprasidone		Oral, Intramuscular
Clozapine	D4>D2 antagonism–> no prolactin effects		used for patients refractory to other treatments	Agranulocytosis, least likely to cause extrapyramidal symptoms. decrease seizure threshold, weight gain, hyperglycemia	Agranulocytosis–> weekly WBC monitoring
Others: sertindole, zotepine

 

Antidepressants:

 

Name	Mechanism of Action	Dosing & route	Indication	Side effects & contraindications	Comments, monitoring etc
Selective serotonin reuptake inhibitors SSRIs:				Sexual dysfunction (decreased libido, impotence, delayed orgasm), anorexia, diarrhea, nervousness, insomnia, hypersensitivity, SIADH–> hyponatremia, slight anticholinergic effects, serotonin syndrome (brainstem 5HT1A receptor hyperstimulation), suicide risk debated. withdrawal syndrome (headache, dizziness, lethargy, nausea)–> taper on withdrawal. Drug interaction: MAOI–> “serotonin syndrome” (hyperthermia, muscle rigidity, abdominal cramping, hypertension, myoclonus, agitation, coma, life-threatening)–> don’t start MAOI for 2 weeks after discontinuing an SSRI, some are metabolised by cyt. P450 Contraindication: mania
Fluoxetine	SSRI	Oral	Depression		active metabolite has a long t1/2–> wait longer after discontinuation
Paroxetine	SSRI	Oral	Depression	more extrapyramidal reactions, mania, risk of congenital malformations CYP2D6 inhibitor
Fluvoxamine	SSRI	Oral	Depression	abnormal LFTs
Sertraline	SSRI	Oral	Depression	Hepatitis
citalopram	SSRI	Oral	Depression		least action on cyt. P450
Escitalopram	SSRI	Oral	Depression
Selective serotonin-noradrenaline reuptake inhibitors (SNRIs):
Venlafaxine	SNRI	Oral, and extended release	Depression	insomnia, headache, agitation, anxiety, SIADH.	Monitor BP
Other antidepressants:
Mirtazapine	Noradrenergic and specific serotonergic antidepressant NaSSA. CNS presynaptic alpha2 antagonist–> increases 5HT & NA release. 5HT2 antagonism–> less sexual side effects, 5HT3 antagonims–> less nausea	Oral		increase appetite, increases cholesterol, sedation (histamine antagonist at lower doses but not at higher doses due to noradrenaline release), hypertension, orthostatic hypotension (a1 antagonist), safe in overdose
Bupropion	Slightly blocks reuptake of NA 5HT & dopamine	Oral		lowers seizure threshold, aggravates psychosis. no anticholinergic, sedating or orthostatic effects
Nefazodone	5HT2 receptor antagonist			somnolence, dizziness, safe in overdose. less side effects than trazodone & less sexual side effects than SSRIs
Trazodone		Oral	Insomnia	priapism, sedation, safe in overdose
Selective noradrenaline reputake inhibitors NARI:
Reboxetine		Oral
Tricyclic antidepressants (TCAs):	Block NA & 5HT reuptake pumps, NB. no effects on adrenaline levels			via M antagonism: tachycardia, dry mouth, constipation, urinary retention & blurred vision. via alpha 1,2 antagonism: postural hypotension. via H1 antagonism: sedation. Also, hallucinations in elderly, cardiac conduction delay, arrythmias. fatal overdose:–> coma, convulsions esp. myoclonic jerks–> rhabdomyolysis, arrhythmias, decreased sweating–> hyperpyrexia. Contraindication: bundle branch block
Despiramine	Tricyclic antidepressant	Oral	Depression		least sedating & anticholenergic of these–> may be used in elderly
Nortryptaline	Tricyclic antidepressant	Oral	Depression		May be used cautiously in elderly
Clomipramine	Tricyclic antidepressant	Oral	Depression, may be used in OCD	Drug interaction: SSRI “serotonin syndrome”
Imipramine	Tricyclic antidepressant, decreases stage 4 sleep–> may be used in bedwetting	Oral	Depression, bedwetting
Amitriptyline	Tricyclic antidepressant	Oral	Depression, migraine & neuropathic pain e.g. fibromyalgia syndrome
Doxepin	Tricyclic antidepressant	Oral	Depression
Mood stabilizers
Lithium salts (lithium carbonate, lithium citrate, different dosages)	probably limits abnormal increase of IP3 in mania	Oral	for acute mania & maintenance & augmentation of depression treatment	Acute: nausea, anorexia, vomiting, diarrhea, ADH antagonism at V2 receptor–> diabetes insipidus–> ployuria, dry mouth, fine tremor. Chronic: cardiotoxcity ECG changes (T wave flattening, conduction delay), hypothyroidism (blocks sysnthesis & release) >hyperthyroidism, renal damage, concentration & memory impairment, tardive dyskinesia, weight gain, glucose intolerane, teratogenic (heart anomalies). Toxicity, levels > 2.0 mmol/l: coarse tremors, ataxia, dysarthria, convulsions, dehydration, renal failure. Narrow Therapeutic Index TI= 0.4 to 0.8 mmol/L–> monitor serum concentrations, Drug Interactions: Diuretics (lower sodium–> increase lithium) & others	Takes 7-10 days to work. Withdraw gradually. monitor serum concentrations, TFTs, U&E & baseline investigations before prescription (U&E, TFT, FBC)
Valproic acid		Oral	acute mania esp. in rapid cycling bipolar disorder & mixed/dysphoric mania	teratogenic, hepatotoxic, hyponatremia.	Monitor Liver enzymes
Lamotrigine		Oral	Bipolar disorder
Carbamazapine		Oral	Bipolar disorder
Monoamine oxidase inhibitors MAOIs:	Inhibits MAO-A & -B–> increases NA & increases 5HT.		Especially useful for atypical depression.	fatal hypertensive crises when foods containing tyramine or certain drugs are ingested, orthostatic hypotension, hepatotoxic, decreased appetite. Tyramine displaces noradrenaline from vesicles–> leaks from terminals–> hypertensive crisis. Drug interactions: SSRIs–> serotonin syndrome–> don’t start SSRI or clomipramine for 3 weeks after discontinuing MAOI many others. (used for atypical/refractory depression & phobias)
Phenelzine	Reversible MAOI	Oral		Dietary/drug restrictions
Isocarboxazid	Reversible MAOI	Oral		Dietary/drug restrictions
Tranycypromine	Reversible MAOI	Oral		Dependence
Moclobemide	Irreversible MAOI-A	Oral	Major depression, phobia	Dietary/drug restrictions

 

CNS depressants & Anxiolytics:

 

Name	Mechanism of Action	Dosing & route	Indication	Side effects & contraindications	Comments, monitoring etc
Benzodiazepines: (whole class)	acts on the benzodiazepine receptor BZR a subunit of GABAA receptor, via increases frequency of Cl- channel opening			Potential for dependence, teratogenic, amnesia, decrease stage 4 sleep–> may be used in night terrors & sleep walking. Muscle relaxant and antiseizure effects as well. Drug interaction Alcohol.	If used for as hypnotic limit it to <10days, if used for anxiety limit to <4-6weeks
Long acting:
Diazepam (trade name-Valium)		Oral, intravenous, rectal	used in status epilepticus, alcohol detoxification/withdrawal
Chlordiazepoxide		Oral	alcohol withdrawal
Prazepam		oral
Intermediate acting:
Lorazepam		Oral	Status epilepticus
Temazepam		Oral
Alprazolam		Oral			fast onset of action–> panic attacks in A&E
Short acting:
Triazolam		Oral	used in insomnia & jet lag
Oxazepam		Oral
Midazolam		Intravenous	Consciouse sedation	#NAME?
Non-benzodiazepines:
Zolpidem	Short acting, acts at BZR a subunit of GABAA receptor, specifically it acts on the w1 subtype of BZR–> no muscle relaxant or antiseizure or deep sleep (stage 3 & 4) effects		Insomnia
Buspirone	5HT1A partial agonist, slow onset of action in weeks, dependence is unlikely, nonsedating	Oral, TID	Generalised anxiety disorder	nausea, headache, dizziness
Zaleplon
Eszopiclone S-enantiomer of zopiclone			transient & chornic insomnia	unpleasant taste
Melatonin receptor agonists:
Melatonin
Ramelteon	MT1 receptor & MT2 receptor on suprachiasmatic nucleus of the hypothalamus		transient & chronic insomnia	hyperprolactinemia	CYP1A2 metabolism
Benzodiazepine receptor antagonists:
Flumazenil			Benzodiazepine overdose

 

CNS stimulants:

 

Name	Mechanism of Action	Dosing & route	Indication	Side effects & contraindications	Comments, monitoring etc
Modafinil	oral a1 agonist, increases glutamate transmission	Oral	Narcolepsy
Pemoline	gradual action	Oral		Hepatic failure	Monitor LFTs
Amfetamines (Amphetamines) & related: Whole class	act on dopamine transporter increases release			Growth retardation–> monitor growth, insomnia, headache, tachycardia, hypertension, Tics, difficulty with ocular accommodation, decreases seizure threshold, exacerbates psychosis, aggression, growth suppression. Contraindication: in hypertension, heart disease (structural or electrical). Drug interaction GI alkalizing agents e.g. antacids, sodium bicarbonate cause increased absorption & toxicity. MAOI hypertensive crisis.	Pretreatment cardiac clinical +/-ECG, Monitor Growth,
Methylphenidate		Oral	Attention-deficit hyperactivity disorder ADHD:	skin conditions, cerebral arteritis
Dexamfetamine (dexamphetamine)		Oral		skin conditions, cerebral arteritis
Sodium oxybate a.k.a. GHB		oral at night	Cataplexy	addictive, sedation, respiratory compromise, confusion, depression, headache Contraindication: sedative hypnotics, alcohol,

 

Opiates & opioids:

 

Name	Mechanism of Action	Dosing & route	Indication	Side effects & contraindications	Comments, monitoring etc
Entire class	Decreases cAMP, open K+ channels & close Ca++ channels,–> inhibit, m= supraspinal analgesia & euphoria–> abuse potential, k= spinal analgesia & dyspohria			!respiratory depression, sedation, nausea, constipation, pruritis,
	– Increases contraction of sphincters (oesophageal, pyloric & ileocecal) & decreases GIT fluid secretion
	– Inhibits substance P release			causes histamine release decreasing BP
Morphine sulphate po as morphine sulphate tablets MST,	See above	oral, intravenous, intrathecal	Pain control. Procedural analgesia.
Fentanyl	very strong at m,	Patch, oral, intravenous, intrathecal
Hydromorphone		oral. intravenous bolus 0.5-2 q3h PRN. intravenous infusion patient controlled analgesia PCA 0.5-1mg/hr
Oxycodone IR immediate release*		Oxycodone IR oral 5-10mg q3h PRN
Oxycontin continuous release*		Contin oral 10-160mg BID
Meperidine* a.k.a. pethidine*	strong m agonist. Some anticholinergic action–> doesn’t cause meiosis unlike the others, may cause mydriasis	intravenous, intrathecal		Contraindication: MAO.	Some anticholinergic action–> doesn’t cause meiosis unlike the others, may cause mydriasis
Methadone,			Opioid withdrawal treatment. Maintenance from opioid withdrawal.
Tramadol *	also inhibits NA & 5HT reuptake in the CNS	oral		!histamine release
Apomorphine	also dopamine agonist at CTZ–> vomiting	Subcutaneous infusion for Parkinson’s disease			also dopamine agonist at CTZ–> vomiting
Codeine *	active metabolite= morphine	oral 30-60mg. If with acetaminophen 15/500, 30/500, 60/500			Use as a cough suppressant & in combination with acetaminophen for pain relief
Dextromethrophan,			Cough suppressant
Loperamide *		oral	anti-diarrheal agent for non-infecious diarrhea		Used for non-infectious diarrhea
Miscellaneous opiates/opioids:	In combinations:
	co-proxamol (dextropropoxyphene +paracetamol), co-codamol (codeine +paracetamol)
	Diphenoxylate (GIT use)
	Tapentadol oral m agonist & inhibits NA reuptake
	propoxyphen
	dihydrocodeine oral s.c. i.m.

 

Drug Dependance:

 

Name	Mechanism of Action	Dosing & route	Indication	Side effects & contraindications	Comments, monitoring etc
Whole class:					NB. think of three things for each drug: mechanism, side effects & overdose, and withdrawal
Stimulants:
Caffeine				insomnia, decreases appetite, increases diuresis, arrhythmias
Nicotine	b2-nicotinic
Cocaine	decreases catecholamine reuptake e.g. dopamine			arrhythmias, hypertension–> cerebral hemorrhage, respiratory arrest, seizures, hyperthermia, coronary vasospasm–> myocardial infarction, chronic use–> dilated cardiomyopathy, nasal ulceration, dilated pupils, psychotic symptoms, aggression, teratogenic. Withdrawal: depression–> suicide. Drug interaction with alcohol to increase the effect of cocaine
Amfetamines (Amphetamines): whole class	Act on dopamine transporter increases release			hyperthermia, necrotising angiitis of cerebral vessels, intracerebral hemorrhage, dilated pupils, psychotic symptoms, aggression, delirium
“Speed” methamphetamine
“Ecstasy” MDMA
Depressants (sedatives): whole class
Ethyl alcohol				Withdrawal a.k.a. delirium tremens (autonomic hyperactivity–> psychotic symptoms–> confusion). Death may occur during withdrawal syndrome (including: seizures & cardiovascular events)
Benzodiazepines				Side effects: respiratory depression–> acidosis/hypoxemia–> coma, aspiration pneumonia & induce cyt. Withdrawal: seizures
Barbiturates: whole class	GABAA enhancer increases duration of Cl- channel opening			Side effects: respiratory depression–> acidosis/hypoxemia–> coma, aspiration pneumonia & induce cyt. P450 CYP 2C9. Withdrawal: seizures
Phenobarbital
Amobarbital
Pentobarbital
Secobarbital
Thiopental/thiopentone
Opiates and opioids (narcotics): whole class	m agonists –> constricted pupils !respiratory/cardiac arrest, diffuse alveolar damage, severe adult & neonatal withdrawal NB. Not teratogenic
Diamorphine a.k.a. Heroin
Methadone
Morphine
Hallucinogens (psychodelics):	Partial agonist of 5HT receptors !psychotic symptoms, flashbacks upto years later
Cannabis/marijuana	acts on CB1 Cannabanoid, THC tetrahydrocannabinol			increases appetite,anti-cholinergic (including memory impairment), amotivational syndrome & lung problems, psychosis, exasorbates schizophrenia
Lysergide LSD	works on 5HT receptors	oral		Psychotic symptoms, hyperthermia
Phencyclidine PCP “angle dust”	blocks NMDA receptor	inh		psychotic symptoms, aggression, hyperthermia, convulsions, coma, rhabdomyolysis, nystagmus
NB ketamine is a PCP analogue
Mescaline (cactus)
Solvents:
Toluene (glue), acetone (nail polish remover), butane (hair spray & lighter fluid)	Lipid soluble (absorbed through lungs–> brain)
Drugs used in treatment:	NB. Detoxification (treating & preventing withdrawal)
Anticraving medication:
Bupropion for smokers (antidepressant)
Naltrexone	blocks dopamine release		for alcoholism
Acamprosate	GABA agonist, NMDA antagonist		for alcoholism
Bromocriptine			for cocaine craving
bromocripine	Dopamine analogues		for cocaine craving
mazindol	Blocking cocaine binding
Methadone (or Levo-alpha acetyl methadyl LAAM)			oral in opioid maintenance programs
Naltrexone & Naloxone	m antagonist		opioid addiction maintains abstinence
Buprenorphine	m agonist/k antagonist	sublingual, patch
Lofexidine	Central a2 agonists: for withdrawal symptoms				less hypotension than Clonidine
Chlordiazepoxide			Benzodiazepine withdrawal
Disulfiram	inhibits acetaldehyde dehydrogenase–> increases acetaldehyde–> increases hangover symptoms			Contraindication: In elderly

 

Miscellaneous medications:

 

Name	Mechanism of Action	Dosing & route	Indication	Side effects & contraindications	Comments, monitoring etc
Amobarbital sodium		Intravenous	to relax patients in interviews for dissociative disorders, conversion disorders & malingering. Also to determine cerebral dominance i.e. Wada test
Sodium lactate or CO2		Inhaled	to induce panic attacks in susceptible people–> used in diagnosis & in cognitive behavioural treatment
Primidone		Oral		vomiting, ataxia,	start at low dose
Tetrabenazine (TBZ)	selectively depletes central monoamines by reversibly binding to the type 2 vesicular monoamine transporter & dopamine receptor blocker	Oral	Huntington disease	akathisia, insomnia, constipation, depression, drooling, and subjective weakness

 
 
 
 

Last modified: December 13, 2015