Neuropharmacology

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!
 


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.


 
 

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