Amitriptyline hydrochloride

CLINICAL USE

Tricyclic antidepressant:

Depression, used especially where

sedation is required

Neuropathic pain

DOSE IN NORMAL RENAL FUNCTION

10–200 mg daily depending on indication

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
313.9

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
96

%Excreted unchanged in urine &nbsp &nbsp :
<2

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :
6–36

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :
9–25/Unchanged

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Dose as in normal renal function

10 to 20 &nbsp &nbsp : Dose as in normal renal function

<10 &nbsp &nbsp &nbsp &nbsp &nbsp :
Dose as in normal renal function

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:
Not dialysed. Dose as in normal renal function

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
Not dialysed. Dose as in normal renal function

HDF/high flux &nbsp :
Unknown dialysability. Dose as in
normal renal function

CAV/VVHD &nbsp &nbsp &nbsp:
Not dialysed. Dose as in normal renal function

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs
Alcohol: increased sedative effect

Analgesics: increased risk of CNS toxicity

with tramadol; possibly increased risk
of side effects with nefopam; possibly
increased sedative effects with opioids

Antiarrhythmics: increased risk of

ventricular arrhythmias with amiodarone
– avoid concomitant use; increased risk
of ventricular arrhythmias with drugs that
prolong the QT interval; increased risk of
arrhythmias with propafenone

Antibacterials: increased risk of

ventricular arrhythmias with moxifloxacin
– avoid concomitant use; concentration
possibly reduced by rifampicin

Anticoagulants: may alter anticoagulant

effect of coumarins

Antidepressants: possibly increased

serotonergic effects with duloxetine;
enhanced CNS excitation and
hypertension with MAOIs and
moclobemide; concentration possibly
increased with SSRIs; concentration
reduced by St John’s wort

Anti-epileptics: convulsive threshold

lowered; concentration reduced by
carbamazepine, primidone, barbiturates
and possibly phenytoin

Antimalarials: avoid concomitant use with

artemether/lumefantrine
Antipsychotics: increased risk of

ventricular arrhythmias especially with
pimozide; increased antimuscarinic
effects with clozapine and phenothiazines;
concentration increased by antipsychotics

Antivirals: increased tricyclic side effects

with amprenavir; concentration possibly
increased with ritonavir
Atomoxetine: increased risk of ventricular

arrhythmias and possibly convulsions
Beta-blockers: increased risk of ventricular

arrhythmias with sotalol

Clonidine: tricyclics antagonise

hypotensive effect; increased risk of
hypertension on clonidine withdrawal

Dopaminergics: avoid use with

entacapone; CNS toxicity reported with
selegiline and rasagiline

Pentamidine: increased risk of ventricular

arrhythmias

Sibutramine: increased risk of CNS

toxicity – avoid concomitant use.

Sympathomimetics: increased risk of

hypertension and arrhythmias with
adrenaline and noradrenaline; metabolism
possibly inhibited by methylphenidate

ADMINISTRATION

Reconstition

–

Route

Oral

Rate of Administration

–

Comments

–

OTHER INFORMATION

Introduce treatment gradually in renal

impairment due to dizziness and postural
hypotension

Withdraw treatment gradually

Anticholinergic side effects: causes urinary

retention, drowsiness, dry mouth, blurred
vision and constipation

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