Generic name (INN)
|
Physicochemistry
[44]
|
Mechanism of action
[45]
|
Routes of administration
[45]
[46]
[47]
|
Pharmacokinetics
[44]
|
Indications
[45]
[46]
[47]
|
Major safety concerns
[45]
[46]
[47]
|
Nonsteroidal anti-inflammatory drugs
|
Unselective agents
|
Aceclofenac
|
Comes in betadex salt and free acid forms; practically insoluble in water, soluble in many organic solvents; degrades on contact with light; phenylacetic acid derivative.
|
As per
diclofenac
.
|
Oral
(PO.)
|
Protein binding > 99%; half-life = 4 hours; metabolised to diclofenac (minor); excretion = urine (67%).
|
As per diclofenac.
|
As per diclofenac.
|
Acemetacin
|
Comes in free form; practically insoluble in water, soluble in certain organic solvents; degrades upon contact with light. Chemically related to
indometacin
|
As per diclofenac.
|
PO.
|
Slightly metabolised to
indometacin
.
|
Rheumatoid arthritis, osteoarthritis and lower back pain.
|
As per diclofenac.
|
Amfenac
|
No available data.
|
As per diclofenac.
|
PO.
|
No data.
|
Pain and inflammation.
|
As diclofenac.
|
Aminophenazone
|
Related to phenylbutazone.
|
As per diclofenac.
|
PO.
|
Not available.
|
Musculoskeletal and joint disorders.
|
Agranulocytosis and cancer.
|
Ampiroxicam
|
Related to piroxicam.
|
As per diclofenac.
|
PO.
|
No data.
|
Rheumatoid arthritis
and
osteoarthritis
.
|
Photosensitivity and other AEs typical of NSAIDs.
|
Amtolmetin guacil
|
Prodrug to
tolmetin
.
|
As per diclofenac.
|
PO.
|
No data.
|
As per diclofenac.
|
As per diclofenac.
|
Aspirin
|
Comes in free form, aluminium and lysine salt forms; fairly insoluble in water (1 in 300); highly soluble (1 in 5) in alcohol; degrades on contact with air. Salicylate.
|
Irreversibly inhibits
COX-1
and
COX-2
; hence inhibiting prostaglandin synthesis.
|
PO, IM, IV, rectal
|
Bioavailability = 80?100%; protein binding = 25?95% (inversely dependent on plasma concentration); half life = 2?3 hours, 15?30 hours (higher doses); excretion = 80?100%.
[48]
|
Blood thinning; mild-to-moderate pain; fever;
rheumatic fever
; migraine;
rheumatoid arthritis
;
Kawasaki's disease
|
GI bleeds; ulcers;
Reye syndrome
; nephrotoxicity; blood dyscrasias (rarely);
Stevens?Johnson syndrome
(uncommon/rare)
|
Azapropazone
|
Comes in free form; fairly insoluble in water and chloroform, soluble in ethanol; phenylbutazone.
|
As per diclofenac.
|
PO, rectal.
|
No data available.
|
Rheumatoid arthritis; gout; ankylosing spondylitis.
|
As per diclofenac.
|
Bendazac
|
Comes in free acid and lysine salt forms. Chemically related to
indometacin
.
|
As per acetametacin.
|
Topical, ophthalmologic.
|
N/A
|
Skin conditions (such as
contact dermatitis
) and
cataracts
.
|
Hepatotoxicity reported.
|
Benorilate
|
Aspirin-paracetamol ester. Practically insoluble in water, sparingly soluble in ethanol and methanol, soluble in acetone and chloroform.
|
As per aspirin and paracetamol.
|
PO.
|
Unavailable.
|
Osteoarthritis; rheumatoid arthritis; soft-tissue rheumatism; mild-moderate pain and fever.
|
As per aspirin and paracetamol.
|
Benzydamine
|
Comes in free acid form; freely soluble in water.
|
As per diclofenac.
|
Topical, PO, rectal, spray and vaginal.
|
No data available.
|
Musculoskeletal disorders; soft-tissue disorders; sore throat.
|
As per diclofenac.
|
Bromfenac
|
Comes in free acid form; phenylacetic acid derivative.
|
Reversible COX-1/COX-2 inhibitor.
|
Ophthalmologic.
|
N/A
|
Postoperative pain and inflammation.
|
Corneal ulceration.
|
Bufexamac
|
Comes in free acid form; practically insoluble in water, soluble in a few organic solvents; degrades upon contact with light.
|
Reversible COX-1/COX-2 inhibition.
|
Topical.
|
No data.
|
Skin disorders.
|
Skin conditions, such as contact dermatitis.
|
Carbasalate
|
Comes in calcium salt form; fairly soluble in water.
|
Is metabolised to aspirin and urea. As per aspirin.
|
Oral.
|
No data.
|
Used for thromboembolic disorders.
|
As per diclofenac.
|
Clonixin
|
Comes in free acid and lysine salt forms.
|
Reversible COX-1/COX-2 inhibition.
|
PO, IM, IV, rectal.
|
No data.
|
Pain.
|
As per diclofenac.
|
Dexibuprofen
|
D-isomer of
ibuprofen
. Propionic acid derivative.
|
As per diclofenac.
|
PO.
|
Bioavailability = ?; protein binding = 99%; metabolism = hepatic via carboxylation and hydroxylation; half-life = 1.8?3.5 hours; excretion = Urine (90%).
[49]
|
Osteoarthritis; mild-moderate pain and menstrual pain.
[50]
|
As per diclofenac.
|
Diclofenac
|
Comes in sodium, potassium and diethylamine (topically used as a gel) salt forms; sparingly soluble in water but soluble in ethanol. Unstable in the presence of light and air. Indole acetic acid derivative.
|
Reversible COX-1/COX-2 inhibitor.
|
PO and topical.
|
Bioavailability = 50?60%; protein binding = 99?99.8%; hepatic metabolism; half-life = 1.2?2 hours; excretion = urine (50?70%), faeces (30?35%)
|
Rheumatoid arthritis
;
osteoarthritis
; inflammatory pain (e.g. period pain); local pain/inflammation (as a gel);
actinic keratoses
; heavy menstrual bleeding
|
As per aspirin, except without Reye syndrome and with the following additions:
myocardial infarctions
,
strokes
and
hypertension
. More prone to causing these AEs compared to the other non-selective NSAIDs.
[51]
|
Diethylamine salicylate
|
Freely soluble in water; degrades upon contact with light and iron.
|
As per diclofenac.
|
Topical.
|
N/A.
|
Rheumatic and musculoskeletal pain.
|
As per bufexamac.
|
Diflunisal
|
Comes in free acid and
arginine
salt forms; practically insoluble in water, soluble in ethanol; degrades upon contact with light.
|
As per diclofenac.
|
PO, IM, IV.
|
Bioavailability = 80?100%; protein binding > 99%; volume of distribution = 0.11 L/kg; hepatic metabolism; half-life = 8?12 hours; excretion = urine (90%), faeces (<5%).
[44]
[52]
|
Pain; osteoarthritis; rheumatoid arthritis.
|
As per diclofenac.
|
Epirizole
|
Comes in free form.
|
As per diclofenac.
|
PO.
|
Not available.
|
Rheumatoid arthritis
.
|
As per diclofenac.
|
Ethenzamide
|
Comes in free form; salicylate.
|
As per diclofenac.
|
PO.
|
Not available.
|
Musculoskeletal pain; fever.
|
As per diclofenac.
|
Etofenamate
|
Liquid; practically insoluble in water, miscible with ethyl acetate and methanol.
|
As per diclofenac.
|
Topical.
|
Not available.
|
Musculoskeletal, joint and soft-tissue disorders.
|
As per bufexamac.
|
Felbinac
|
Comes in free and
diisopropanolamine
salt forms; practically insoluble in water and ethanol, soluble in methanol.
|
As per diclofenac.
|
Topical.
|
N/A
|
Musculoskeletal pain and soft tissue injuries.
|
As per bufexamac.
|
Fenbufen
|
Comes as free acid; fairly insoluble in most solvents (including water); propionic acid derivative.
|
As per diclofenac.
|
PO.
|
Protein binding > 99%; half-life = 10?17 hours.
|
As per diclofenac.
|
As per diclofenac.
|
Fenoprofen
|
Comes in calcium salt; fairly insoluble in water and chloroform and fairly soluble in alcohol; sensitive to degradation by air. Propionic acid derivative.
|
As per diclofenac.
|
PO.
|
Bioavailability = ?; protein binding = 99%; hepatic metabolism; excretion = urine, faeces.
[53]
|
Pain; rheumatoid arthritis and osteoarthritis.
|
As per diclofenac.
|
Fentiazac
|
Comes in free form and calcium salt; acetic acid derivative.
|
As per diclofenac.
|
PO.
|
No data.
|
As per diclofenac.
|
As per diclofenac.
|
Fepradinol
|
Comes in free acid and hydrochloride salt forms.
|
As per diclofenac.
|
Topical.
|
N/A
|
Local inflammatory response.
|
As per bufexamac.
|
Feprazone
|
Comes in free acid and piperazine salt forms. Phenylbutazone.
|
As per diclofenac.
|
PO, Rectal, topical.
|
Not available.
|
As per diclofenac.
|
As per bufexamac (topical use) and diclofenac (PO/rectal).
|
Floctafenine
|
Comes in free acid form; anthranilic acid derivative.
|
As per diclofenac.
|
Oral.
|
Extensively metabolised by the liver; half-life = 8 hours; excretion = urinary and biliary.
|
Short-term relief from pain.
|
As per diclofenac.
|
Flufenamic acid
|
Comes in free acid form and aluminium salt form; anthranilic acid.
|
As per diclofenac.
|
Topical.
|
N/A
|
Soft tissue inflammation and pain.
|
As per bufexamac.
|
Flurbiprofen
|
Comes in sodium salt and free acid forms; fairly insoluble in water but soluble in ethanol; sensitive to degradation by air. Propionic acid derivative.
|
As per diclofenac.
|
PO, IM, IV, ophthalmologic.
|
Bioavailability = 96% (oral); protein binding > 99%; volume of distribution = 0.12 L/kg; excretion = urine (70%).
[54]
|
Ophthalmologic:
Vernal keratoconjunctivitis
; postoperative ocular swelling; herpetic stromal keratitis, excimer laser photorefractive keratectomy; ocular gingivitis. Systemic use:
rheumatoid arthritis
;
osteoarthritis
.
[54]
|
As per bromfenac (ophthalmologic) and diclofenac (PO/IM/IV).
|
Glucametacin
|
Indometacin derivative.
|
As per diclofenac.
|
PO.
|
Not available.
|
Musculoskeletal, joint, peri-articular and soft-tissue disorders.
|
As per diclofenac.
|
Ibuprofen
|
Comes in lysine salt and free acid forms; practically insoluble in water, but soluble in ethanol,
acetone
,
methanol
,
dichloromethane
and
chloroform
. Degrades in the presence of air. Propionic acid derivative.
|
As per diclofenac.
|
PO, IV, topical
|
Bioavailability = 80?100%; protein binding = 90?99%; hepatic metabolism, mostly via
CYP2C9
and
CYP2C19
-mediated oxidation; excretion = Urine (50?60%), faeces.
[55]
|
Pain; fever; inflammatory illness;
rheumatoid arthritis
;
osteoarthritis
; heavy menstrual bleeding;
patent ductus arteriosus
.
[46]
[56]
[57]
|
As per diclofenac, except with lower risk of myocardial infarction, stroke and hypertension.
|
Imidazole salicylate
|
Comes in free form. Salicylate.
|
As per diclofenac.
|
PO, rectal, topical.
|
Not available.
|
Muscular and rheumatic pain.
|
As per bufexamac (topical use) and diclofenac (PO/rectal).
|
Indometacin
|
Comes in free acid and sodium salt forms; practically insoluble in water and most solvents; sensitive to degradation by light. Acetic acid derivative.
|
As per diclofenac.
|
PO, IV, rectal
|
Bioavailability = 100% (oral); protein binding = 90%; hepatic metabolism; excretion = urine (60%), faeces (33%).
[58]
|
Rheumatoid arthritis
;
osteoarthritis
;
gout
;
ankylosing spondylitis
; period pain; patent ductus arteriosus.
[46]
|
As per diclofenac.
|
Isonixin
|
Comes in free form.
|
As per diclofenac.
|
PO, rectal and topical.
|
Not available.
|
Musculoskeletal and joint disorders.
|
As per bufexamac (topical use) and diclofenac (PO/rectal).
|
Kebuzone
|
Comes in free and sodium salt form; phenylbutazone derivative.
|
As per diclofenac.
|
IM, PO.
|
Not available.
|
As per diclofenac.
|
As per diclofenac.
|
Ketoprofen
|
Comes in free acid, lysine salt, sodium salt and hydrochloride salt forms; the dex-enantiomer comes in
trometamol
salt form. Practically insoluble in water; freely soluble in most other solvents. Propionic acid derivative.
|
As per diclofenac.
|
PO, rectal, topical, transdermal, intravenous, intramuscular.
[59]
[60]
|
Bioavailability > 92% (oral), 70?90% (rectal); protein binding > 99%; volume of distribution = 0.1?0.2 L/kg; hepatic metabolism; half-life = 1.5?2 hours (oral), 2.2 hours (rectal), 2 hours (intravenous).
[61]
[62]
|
Rheumatoid arthritis
,
osteoarthritis
and superficial sporting injuries (topical use).
[46]
[63]
|
As per diclofenac.
|
Ketorolac
|
Comes in the
trometamol
salt form; highly soluble in water. Degrades in the presence of light. Acetic acid derivative.
|
As per diclofenac.
|
PO, IM, IV, intranasal, tromethamine and ophthalmologic.
|
Bioavailability of IM formulation = 100%; protein binding = 99%; hepatic metabolism mostly via glucoronic acid conjugation and p-hydroxylation; half-life = 5?6 hours; excretion = urine (91.4%), faeces (6.1%).
[64]
|
Mild-moderate postoperative pain; acute migraine; inflammation of the eye due to cataract surgery or allergic seasonal
conjunctivitis
; prevention of acute pseudophakic cystoid macular oedema.
[65]
[66]
[67]
[68]
[69]
[70]
[71]
|
As per diclofenac.
|
Lornoxicam
|
Hydrochloride salt form used; oxicam derivative.
|
As per diclofenac.
|
PO.
|
Protein binding = 99%; volume of distribution = 0.2 L/kg; half-life = 3?5 hours; excretion = faeces (51%), urine (42%).
[72]
[73]
|
Acute and chronic pain.
|
As per diclofenac.
|
Loxoprofen
|
Comes in sodium salt form. Propionic acid derivative.
|
As per diclofenac.
|
Topical.
|
N/A
|
Local inflammation and pain.
|
As per diclofenac.
|
Magnesium salicylate
|
Comes in free form; soluble in water and ethanol; salicylate.
|
As per diclofenac.
|
PO.
|
Not available.
|
As per diclofenac.
|
As per diclofenac.
|
Meclofenamic acid
|
Comes in free acid and sodium salt form, sodium salt is the form used in human medicine; practically insoluble in water (free acid) and freely soluble in water (sodium salt); sensitive to degradation by air and light.
|
As per diclofenac.
|
PO.
|
Protein binding > 99%; half-life = 2?4 hours; hepatically metabolised via oxidation, hydroxylation, dehalogenation and conjugation with glucuronic acid; excretion = urine, faeces (20?30%).
[44]
|
Osteoarthritis; rheumatoid arthritis; mild-moderate pain; dysmenorrhoea;
menorrhagia
.
|
As per diclofenac.
|
Mefenamic acid
|
Comes in free acid form; practically insoluble in water, fairly insoluble in organic solvents; degrades on contact with air and light. Anthranilic acid derivative.
|
As per diclofenac.
|
PO.
|
Protein binding extensive; hepatic metabolism, mostly via
CYP2C9
; half-life = 2 hours; excretion = urine (66%), faeces (20?25%).
[74]
|
Inflammatory pain and heavy menstrual bleeding.
[46]
|
As per diclofenac.
|
Mofezolac
|
Comes in free form.
|
As per diclofenac.
|
PO.
|
Not available.
|
Musculoskeletal and joint pain.
|
As per diclofenac.
|
Morniflumate
|
Comes in free acid form; niflumic acid derivative.
|
As per diclofenac.
|
PO, rectal.
|
Not available.
|
Inflammatory conditions.
|
As per diclofenac.
|
Nabumetone
|
Comes in free acid form; practically insoluble in water, freely soluble in acetone; degrades on contact with air and light.
|
As per diclofenac.
|
PO.
|
Protein binding = 99%; hepatically metabolised; half-life = 24 hours; excretion = urine (80%), faeces (9%).
[75]
|
Osteoarthritis; rheumatoid arthritis.
|
As per diclofenac.
|
Naproxen
|
Comes in free acid and sodium form; practically insoluble in water in free form, freely soluble in water (sodium salt), fairly soluble in most organic solvents. Degrades on contact with air and light. Propionic acid derivative.
|
As per diclofenac.
|
PO.
|
Bioavailability = ?; protein binding > 99.5%; volume of distribution = 10% of bodyweight; half-life = 12?15 hours; excretion = urine (95%), faeces (<3%).
[76]
|
Rheumatoid arthritis; osteoarthritis; ankylosing spondylitis;
juvenile idiopathic arthritis
; inflammatory pain; heavy menstrual bleeding.
|
As per diclofenac. less prone to causing thrombotic events compared to other non-selective NSAIDs.
[51]
|
Nepafenac
|
Comes in free form; related to amfenac.
|
As per diclofenac.
|
Ophthalmologic.
|
Unavailable.
|
Inflammation and pain following cataract surgery.
|
As per bromfenac.
|
Niflumic acid
|
Comes in free acid form, glycinamide and ethyl ester form; practically insoluble in water, soluble in ethanol, acetone and methanol. Nicotinic acid derivative.
|
As per diclofenac.
|
PO, rectal (ethyl ester,
morniflumate
).
|
Unavailable.
|
Musculoskeletal, joint and mouth inflammatory disorders.
|
As per diclofenac.
|
Oxaprozin
|
Comes in potassium and free acid forms; degrades upon contact with light. Propionic acid derivative.
|
As per diclofenac.
|
PO.
|
Bioavailability = ?; protein binding > 99.5%; volume of distribution = 0.15?0.25 L/kg; half-life = 50?60 hours; excretion = urine (65), faeces (35%).
[77]
[78]
|
Osteoarthritis; rheumatoid arthritis.
|
As per diclofenac.
|
Oxyphenbutazone
|
Comes in free form. Phenylbutazone.
|
As per diclofenac.
|
PO, Ophthalmologic.
|
Unavailable.
|
Ophthalmologic:
Episcleritis
. Systemic (now seldom used due to adverse effects): ankylosing spondylitis; rheumatoid arthritis; osteoarthritis.
|
As per bromfenac. For systemic use haematological side effects such as aplastic anaemia; agranulocytosis; leucopenia; neutropenia; etc.
|
Phenazone
|
No data.
|
As per diclofenac.
|
PO,
otolaryngologic
.
|
Protein binding < 10%; half-life = 12 hours; hepatic metabolised; excretion = urine (primary), faeces.
|
Acute
otitis media
.
|
Nephrotoxicity and haematologic toxicity and other AEs typical of NSAIDs.
|
Phenylbutazone
|
Comes in free form; practically insoluble in water, freely soluble in most organic solvents; degrades upon contact with light and air.
|
As per diclofenac.
|
PO, rectal, topical.
|
No data available.
|
Ankylosing spondylitis; acute gout; osteoarthritis; rheumatoid arthritis.
|
Haematologic toxicity (including agranulocytosis, aplastic anaemia) and AEs typical of NSAIDs.
|
Piketoprofen
|
Comes in free form.
|
As per diclofenac.
|
Topical.
|
N/A.
|
Musculoskeletal, joint, peri-articular and soft-tissue disorders.
|
As per other topical NSAIDs.
|
Piroxicam
|
Comes in free acid and betadex salt forms; practically insoluble in water, slightly soluble in ethanol; degrades on contact with air and light. Enolic acid derivative.
|
As per diclofenac.
|
PO, topical.
|
Protein binding = 99%; extensively hepatically metabolised; half-life = 36?45 hours; excretion = urine, faeces.
[79]
[80]
|
Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis and sports injuries (topical use).
[46]
|
As per diclofenac.
|
Proglumetacin
|
Comes in maleate salt form; indometacin derivative.
|
As per diclofenac.
|
PO, rectal, topical.
|
Not available.
|
Musculoskeletal and joint disorders.
|
As per diclofenac.
|
Proquazone
|
Comes in free form.
|
As per diclofenac.
|
PO, rectal.
|
Not available.
|
As per diclofenac.
|
As per diclofenac.
|
Pranoprofen
|
No data.
|
As per diclofenac.
|
PO, ophthalmologic.
|
Not available.
|
Pain, inflammation and fever.
|
As per diclofenac.
|
Salamidacetic acid
|
Comes in sodium and diethylamine salt forms; salicylate.
|
As per diclofenac.
|
PO.
|
Unavailable.
|
Musculoskeletal disorders.
|
As per diclofenac.
|
Salicylamide
|
Fairly insoluble in water and chloroform; soluble in most other organic solvents; salicylate.
|
As per diclofenac.
|
PO, topical.
|
No data.
|
Muscular and rheumatic diseases.
|
As per diclofenac.
|
Salol
|
No data.
|
As per diclofenac.
|
PO, topical.
|
No data.
|
Lower urinary tract infections.
|
As per diclofenac.
|
Salsalate
|
Degrades upon contact with air; salicylate derivative.
|
As per diclofenac.
|
PO.
|
Hepatic metabolism; half-life = 7?8 hours; excretion = urine.
[81]
|
Rheumatoid arthritis, osteoarthritis.
|
As per diclofenac.
|
Sodium salicylate
|
Freely soluble in water; degrades upon contact with air and light; salicylate.
|
As per diclofenac.
|
PO, IV, topical.
|
No data.
|
Pain, fever and rheumatic conditions.
|
Cardiac problems; otherwise As per diclofenac.
|
Sulindac
|
Comes in free acid and sodium salt forms; practically insoluble in water and hexane, very slightly soluble in most organic solvents. Degrades upon contact with light. Acetic acid derivative.
|
As per diclofenac.
|
PO, rectal.
|
Bioavailability = 90%; protein binding = 93% (sulindac), 98% (active metabolite); hepatic metabolism; excretion = urine (50%), faeces (25%).
[82]
|
Rheumatoid arthritis; osteoarthritis; gout; ankylosing spondylitis; inflammatory pain.
[46]
|
As per diclofenac.
|
Suxibuzone
|
Practically insoluble in water, soluble in ethanol and acetone; phenylbutazone.
|
As per diclofenac.
|
PO, topical.
|
No data.
|
Musculoskeletal and joint disorders.
|
As per phenylbutazone.
|
Tenoxicam
|
Comes as free acid; practically insoluble in water, fairly insoluble in organic solvents; degrades upon contact with light.
|
As per diclofenac.
|
PO, rectal.
|
Bioavailability = 100% (oral), 80% (rectal); protein binding = 99%; volume of distribution = 0.15 L/kg; half-life = 60?75 hours; excretion = urine (67%), faeces (33%).
[83]
|
Osteoarthritis; rheumatoid arthritis; soft tissue injury.
|
As per diclofenac.
|
Tetridamine
|
No data.
|
As per diclofenac.
|
Vaginal.
|
No data.
|
Vaginitis
.
|
As per diclofenac.
|
Tiaprofenic acid
|
Comes as free acid; practically insoluble in water but freely soluble in most organic solvents; propionic acid derivative; degrades upon contact with light. Propionic acid derivative.
|
As per diclofenac.
|
PO.
|
Protein binding > 99%; volume of distribution = 0.1?0.2 L/kg; hepatic metabolism; half-life = 2?4 hours.
[84]
|
Ankylosing spondylitis; osteoarthritis; rheumatoid arthritis; fibrosis; capsulitis; soft-tissue disorders.
|
As per diclofenac.
|
Tiaramide
|
No data.
|
As per diclofenac.
|
PO.
|
No data.
|
Pain; inflammation.
|
As per diclofenac.
|
Tinoridine
|
No data.
|
As per diclofenac.
|
No data.
|
No data.
|
Pain; inflammation.
|
As per diclofenac.
|
Tolfenamic acid
|
Comes as free acid; practically insoluble in water; degrades upon contact with light; anthranilic acid.
|
As per diclofenac.
|
PO.
|
Protein binding = 99%; half-life = 2 hours; hepatically metabolised; excretion = urine (90%), faeces.
|
Migraine; osteoarthritis; rheumatoid arthritis; dysmenorrhoea.
|
As per diclofenac.
|
Tolmetin
|
Comes in sodium salt form; freely soluble in water, slightly soluble in ethanol, freely soluble in methanol. Acetic acid derivative.
|
As per diclofenac.
|
PO.
|
Protein binding > 99%; volume of distribution = 7?10 L; half-life = 1 hour; excretion = urine (90%).
[85]
|
Osteoarthritis; rheumatoid arthritis.
|
As per diclofenac.
|
Ufenamate
|
No data.
|
No data.
|
Topical.
|
No data.
|
Inflammatory skin disorders.
|
As per other topical NSAIDs.
|
COX-2 selective inhibitors
|
Celecoxib
|
Comes in free form; practically insoluble in water, fairly soluble in organic solvents. Degrades on contact with light and moisture.
Sulfonamide
.
|
Selective COX-2 inhibitor.
|
PO.
|
Protein binding = 97%; hepatic metabolism, mostly via
CYP2C9
; faeces (57%), urine (27%).
[86]
|
Rheumatoid arthritis; osteoarthritis; ankylosing spondylitis; pain due to dysmenorrhoea or injury.
|
As per non-selective NSAIDs. More prone to causing thrombotic events than most of them, however, except diclofenac.
|
Etodolac
|
Comes in free form; practically insoluble in water, freely soluble in acetone and dehydrated alcohol. Acetic acid derivative.
|
As per celecoxib.
|
PO.
|
Bioavailability = ?; protein binding > 99%; volume of distribution = 0.41 L/kg; half-life = 6?7 hours; excretion = urine (73%).
[87]
[88]
[89]
|
Rheumatoid arthritis, including juvenile idiopathic arthritis; osteoarthritis; acute pain.
|
As per diclofenac.
|
Etoricoxib
|
Comes in free form;
sulfonamide
.
|
As per celecoxib.
|
PO.
|
Bioavailability = 100%; protein binding = 91.4%; volume of distribution = 120 L; half-life = 22 hours; hepatic metabolism; excretion = urine (70%), faeces (20%).
[90]
|
Acute pain; gout; osteoarthritis.
|
As per diclofenac.
|
Lumiracoxib
†
|
Comes in free form; acetic acid derivative.
|
As per celecoxib.
|
PO.
|
Bioavailability = 74%; protein binding > 98%; extensive hepatic metabolism, mostly via
CYP2C9
; half-life = 3?6 hours; excretion = Urine (50%), faeces (50%).
[91]
|
Osteoarthritis.
|
As above, plus hepatotoxicity.
|
Meloxicam
|
Comes in free form; fairly insoluble in water and in most organic solvents; oxicam derivative.
|
As per celecoxib.
|
PO, rectal.
|
Bioavailability = 89%; protein binding > 99%; volume of distribution = 0.1?0.2 L/kg; half-life = 22?24 hours; extensive hepatic metabolism; excretion = urine (45%), faeces (47%).
[92]
|
Osteoarthritis; rheumatoid arthritis.
|
As per diclofenac.
|
Nimesulide
|
Comes in free and betadex form; practically insoluble in water and ethanol, soluble in acetone.
|
As per celecoxib.
|
PO, rectal, topical.
|
Unavailable.
|
Acute pain; dysmenorrhoea; sprains (topical);
tendinitis
.
|
As per diclofenac.
|
Parecoxib
|
Comes in sodium salt form; sulfonamide.
|
As per celecoxib.
|
IM, IV.
|
Plasma binding = 98%; volume of distribution = 55 L; hepatic metabolism, mostly via
CYP2C9
,
CYP3A4
; half-life = 8 hours; excretion = urine (70%).
[93]
|
Postoperative pain.
|
As per diclofenac.
|
Rofecoxib
†
|
Comes in free form; sulfonamide.
|
As per celecoxib.
|
PO.
|
Bioavailability = 93%; protein binding = 87%; hepatic metabolism; half-life = 17 hours.
[94]
[95]
|
Acute pain; osteoarthritis; rheumatoid arthritis.
|
As per diclofenac.
|
Valdecoxib
†
|
Comes in free form; sulfonamide.
|
As per celecoxib.
|
PO.
|
Bioavailability = 83%; protein binding = 98%; hepatic metabolism, mostly via
CYP3A4
and
CYP2C9
; half-life = 8.11 hours; excretion = urine (90%).
[96]
|
Pain from
dysmenorrhoea
; rheumatoid arthritis; osteoarthritis.
|
As above and also potentially fatal skin reactions (e.g.
toxic epidermal necrolysis
).
|
Opioids
|
Those with a morphine skeleton
|
Buprenorphine
|
Comes in free and hydrochloride salt forms; fairly insoluble in water, soluble in ethanol, methanol and acetone; degrades upon contact with light.
|
Partial agonist at the mu opioid receptor; agonist at delta opioid receptor; antagonist at kappa opioid receptor.
|
Sublingual, transdermal, IM, IV, intranasal, epidural, SC.
|
Bioavailability = 79% (sublingual); protein binding = 96%: volume of distribution = 97?187 L/kg; half-life = 20?36 hours; excretion = urine, faeces.
[97]
|
Opioid dependence, moderate-severe pain.
|
As per codeine, respiratory effects are subject to a ceiling effect.
|
Codeine
|
Comes in free form, hydrochloride salt, sulfate salt and phosphate salts; soluble in boiling water (free form), freely soluble in ethanol (free form), soluble/freely soluble in water (salt forms); sensitive to degradation by light. Methoxy analogue of morphine.
|
Metabolised to morphine, which activates the
opioid receptors
.
|
PO, IM, IV.
|
Extensive hepatic metabolism, mostly via
CYP2D6
, to
morphine
; half-life = 3?4 hours; excretion = urine (86%).
[98]
|
Mild-moderate pain, often in combination with
paracetamol
or
ibuprofen
.
|
Constipation, dependence, sedation, itching, nausea, vomiting and respiratory depression.
|
Diamorphine
|
Comes in hydrochloride salt form; freely soluble in water, soluble in alcohol; degrades upon contact with light. Diacetyl derivative of morphine.
|
Rapidly hydrolysed to 6-acetylmorphine and then to morphine after crossing the blood-brain barrier which in turn activates the opioid receptors in the CNS.
|
IM, intrathecal, intranasal, PO, IV, SC.
|
Extensively metabolised to morphine with 6-acetylmorphine as a possible intermediate. Mostly excreted in urine.
|
Severe pain (including labour pain); cough due to terminal lung cancer; angina; left ventricular failure.
|
As per codeine. Higher potential for abuse compared to other opioids due to its rapid penetration of the blood-brain barrier.
|
Dihydrocodeine
|
Comes in freebase, hydrochloride, phosphate, polistirex, thiocyanate, tartrate, bitartrate and hydrogen tartrate salt forms; freely soluble in water, practically insoluble in organic solvents (hydrogen tartrate salt); degrades upon contact with air and light.
|
Opioid receptor agonist.
|
IM, IV, PO, SC.
|
Bioavailability = 20%; extensive hepatic metabolism, partly via
CYP2D6
to
dihydromorphine
and
CYP3A4
to
nordihydrocodeine
; half-life = 3.5 ?5 hours; excretion = urine.
|
Moderate-severe pain; usually in combination with paracetamol and/or aspirin.
|
As per codeine.
|
Ethylmorphine
|
Comes in freebase, hydrochloride, camphorate and camsilate salt forms; soluble in water and alcohol; degrades upon contact with light.
|
Opioid receptor ligand.
|
PO.
|
No data.
|
Cough suppressant.
|
As per codeine.
|
Hydrocodone
|
Comes in hydrochloride/tartrate salt form; freely soluble in water, practically insoluble in most organic solvents; degrades upon contact with light/air.
|
Opioid receptor ligand.
|
PO.
|
Protein binding = 19%; extensively hepatically metabolised, mostly via
CYP3A4
, but via
CYP2D6
to a lesser extent to
hydromorphone
; half-life = 8 hours; excretion = urine.
[99]
|
Chronic pain.
|
As per codeine.
|
Hydromorphone
|
Comes in hydrochloride salt form; freely soluble in water, fairly insoluble in organic solvents; degrades upon contact with light or temperatures outside 15 °C and 35 °C.
|
Opioid receptor agonist.
|
IM, IV, PO, SC.
|
Bioavailability = 50?62% (oral); protein binding = 8?19%; extensively hepatically metabolised; half-life = 2?3 hours; excretion = urine.
[100]
|
Moderate-severe pain; cough.
|
As per codeine.
|
Morphine
|
Comes in freebase form, hydrochloride salt, sulfate salt and tartrate salt forms; soluble in water; degrades in the presence of light.
|
Opioid receptor agonist (μ, δ, κ).
|
IM, intrathecal, PO, IV, SC, rectal.
|
Protein binding = 35%; extensive hepatic metabolism, with some metabolism occur in the gut after oral administration; half-life = 2 hours; excretion = urine (90%).
|
Moderate-severe pain.
|
As per codeine.
|
Nicomorphine
|
Di
nicotinic acid
ester derivative of morphine.
|
As per morphine.
|
IM, IV, PO, rectal, SC.
|
No available data.
|
Moderate-severe pain.
|
As per codeine.
|
Oxycodone
|
Comes in freebase, hydrochloride and
terephthalate
salt forms; freely soluble in water and practically insoluble in organic solvents; degrades upon contact with air.
|
Opioid receptor agonist.
|
PO.
|
Bioavailability = 60?87%; protein binding = 45%; volume of distribution = 2.6 L/kg; extensively metabolised in the liver via
CYP3A4
and to a lesser extent via
CYP2D6
to
oxymorphone
; half-life = 2?4 hours; excretion = urine (83%).
[101]
|
Moderate-severe pain.
|
As per codeine.
|
Oxymorphone
|
Comes in hydrochloride salt form; fairly soluble in water (1 in 4), practically insoluble in most organic solvents; degrades upon contact with air, light and temperatures outside 15 °C to 30 °C.
|
As per morphine.
|
PO, IM, SC.
|
Bioavailability = 10% (oral); protein binding = 10?12%; volume of distribution = 1.94?4.22 L/kg; hepatic metabolism; half-life = 7?9 hours, 9?11 hours (XR); excretion = urine, faeces.
[102]
|
Postoperative analgesia/anaesthesia; moderate-severe pain.
|
As per codeine.
|
Morphinans
|
Butorphanol
|
Comes in tartrate salt form; sparingly soluble in water, insoluble in most organic solvents; degrades upon contact with air and at temperatures outside the range of 15 °C and 30 °C.
|
Kappa opioid receptor agonist; mu opioid receptor partial agonist.
|
IM, IV, intranasal.
|
Bioavailability = 60?70% (intranasal); protein binding = 80%; volume of distribution = 487 L; hepatic metabolism, mostly via hydroxylation; excretion = urine (mostly); half-life = 4.6 hours.
[103]
|
Moderate-severe pain, including labour pain.
|
As above, but with a higher propensity for causing hallucinations and delusions. Respiratory depression is subject to ceiling effect.
|
Levorphanol
|
Comes in tartrate salt form; fairly insoluble in water (1 in 50) and fairly insoluble in ethanol, chloroform and ether; unstable outside of 15 °C and 30 °C; phenanthrene derivative.
|
Mu opioid; NMDA antagonist;
SNRI
.
[104]
|
PO, IM, IV, SC.
|
Protein binding = 40%; extensive first-pass metabolism; half-life = 12?16 hours, 30 hours (repeated dosing).
[104]
[105]
|
Acute/chronic pain.
|
As per codeine.
|
Nalbuphine
|
Comes primarily as its hydrochloride salt.
|
Full agonist at
kappa opioid receptors
, partial agonist/antagonist at the
mu opioid receptors
.
[44]
|
IM, IV, SC.
|
Protein binding = not significant; hepatic metabolism; half-life = 5 hours; excretion = urine, faeces.
[106]
[107]
|
Pain; anaesthesia supplement; opioid-induced pruritus.
|
As per codeine. Respiratory depression is subject to ceiling effect.
|
Benzomorphans
|
Dezocine
|
No data available.
|
Mixed opioid agonist-antagonist.
|
IM, IV.
|
Volume of distribution = 9?12 L/kg; half-life = 2.2?2.7 hours.
|
Moderate-severe pain.
|
As per codeine.
|
Eptazocine
|
Comes as hydrobromide salt.
|
As per morphine.
|
IM, SC.
|
No data.
|
Moderate-severe pain.
|
As per codeine.
|
Pentazocine
|
Comes in free, hydrochloride and lactate salt forms; fairly insoluble in water (1:30 or less), more soluble in ethanol and chloroform; degrades upon contact with air and light.
|
Kappa opioid receptor agonist; mu opioid receptor antagonist/partial agonist.
|
IM, IV, SC.
|
Bioavailability = 60?70%; protein binding = 60%; hepatic metabolism; half-life = 2?3 hours; excretion = urine (primary), faeces.
[108]
[109]
|
Moderate-severe pain.
|
As per codeine. Respiratory effects are subject to a ceiling effect.
|
Phenylpiperidines
|
Anileridine
|
Comes in free, hydrochloride and phosphate forms; fairly insoluble in water, soluble in ethanol, ether and chloroform; degrades upon contact with air and light.
|
Mu opioid receptor agonist.
|
IM, IV.
|
No data.
|
Moderate-severe pain.
|
As per codeine.
|
Ketobemidone
|
Comes in hydrochloride salt form; freely soluble in water, soluble in ethanol and fairly insoluble in
dichloromethane
.
|
Mu opioid; NMDA antagonist.
|
PO, IM, IV, rectal.
|
Bioavailability = 34% (oral), 44% (rectal); half-life = 2?3.5 hours.
[110]
|
Moderate-severe pain.
|
As per other opioids.
|
Pethidine
|
Comes in hydrochloride form; very soluble in water, sparingly soluble in ether, soluble in ethanol; degrades upon contact with air and light.
|
Mu opioid receptor agonist with some serotonergic effects.
|
IM, IV, PO, SC.
|
Bioavailability = 50?60%; protein binding = 65?75%; hepatic metabolism; half-life = 2.5?4 hours; excretion = urine (primarily).
[111]
[112]
[113]
[114]
[115]
|
Moderate-severe pain.
|
As per other opioids; and seizures, anxiety, mood changes and
serotonin syndrome
.
|
Open-chain opioids
|
Dextromoramide
|
Comes in tartrate salt and free forms; soluble in water (tartrate salt).
|
Mu opioid.
|
IM, IV, PO, rectal.
|
No data available.
|
Severe pain.
|
As per other opioids.
|
Dextropropoxyphene
|
Comes in free form, hydrochloride and napsilate salt forms; very soluble in water (HCl), practically insoluble in water (napsilate); degrades upon contact with light and air.
|
Mu opioid.
|
PO.
|
Protein binding = 80%; hepatic metabolism; half-life = 6?12 hours, 30?36 hours (active metabolite).
|
Mild-moderate pain.
|
As per other opioids, plus ECG changes.
|
Dipipanone
|
Comes in hydrochloride salt form; practically insoluble in water and ether, soluble in acetone and ethanol.
|
Mu opioid.
|
PO, often in combination with
cyclizine
.
|
Half-life = 20 hours.
[116]
|
Moderate-severe pain.
|
Less sedating than morphine, otherwise as per morphine.
|
Levacetylmethadol
†
|
Comes in hydrochloride salt form.
|
As above plus nicotinic acetylcholine receptor antagonist.
|
PO.
|
Protein binding = 80%; half-life = 2.6 days.
|
Opioid dependence.
|
As per other opioids, plus ventricular rhythm disorders.
|
Levomethadone
|
Comes in hydrochloride salt form; soluble in water and alcohol; degrades upon contact with light.
|
Mu opioid; NMDA antagonist.
|
PO.
|
No data.
|
As per methadone.
|
As per methadone.
|
Meptazinol
|
Comes in hydrochloride salt form; soluble in water, ethanol and methanol, fairly insoluble in acetone; unstable at temperatures greater than 25 °C.
|
Mixed opioid agonist-antagonist, partial agonist at mu-1 receptor; cholinergic actions exist.
|
IM, IV, PO.
|
Bioavailability = 8.69% (oral); protein binding = 27.1%; half-life = 2 hours; excretion = urine.
[117]
|
Moderate-severe pain; perioperative analgesia;
renal colic
.
|
As per pentazocine.
|
Methadone
|
Comes in hydrochloride salt form; soluble in water and ethanol; degrades upon contact with air and light and outside the temperature range of 15 °C and 30 °C.
|
Mu opioid; NMDA antagonist.
|
IM, IV, PO, SC.
|
Bioavailability = 36?100% (mean: 70?80%); protein binding = 81?97% (mean: 87%); volume of distribution = 1.9-8 L/kg (mean: 4 L/kg); hepatic metabolism, mostly via
CYP3A4
,
CYP2B6
and to a lesser extent:
CYP2C9
,
CYP2C19
,
CYP2D6
&
CYP2C8
; half-life = 5?130 hours (mean: 20?35 hours); excretion = urine (20?50%), faeces.
[118]
|
Opioid addiction; chronic pain.
|
As per other opioids, plus QT interval prolongation.
|
Piritramide
|
Comes in free or tartrate salt forms.
|
Mu opioid.
|
IM, IV, SC.
|
No data available.
|
Severe pain.
|
As per other opioids.
|
Tapentadol
|
Comes in free and hydrochloride salt forms.
|
Mu opioid and norepinephrine reuptake inhibitor.
|
PO.
|
Bioavailability = 32%; protein binding = 20%; hepatic metabolism, mostly via
CYP2C9
,
CYP2C19
,
CYP2D6
; excretion = urine (70%), faeces; half-life = 4 hours.
|
Moderate-severe pain.
|
As per other opioids; less likely to cause nausea, vomiting and constipation.
|
Tilidine
|
Comes in hydrochloride salt form; soluble in water, ethanol and dichloromethane; degrades upon contact with light.
|
Mu opioid metabolite,
nortilidine
.
|
PO.
|
No data.
|
Moderate-severe pain.
|
As per other opioids.
|
Tramadol
|
Comes in hydrochloride salt form; freely soluble in water and methanol, insoluble in acetone; degrades at temperatures less than 15 °C and 30 °C and upon contact with light.
|
Mu opioid (mostly via its active metabolite,
O-desmethyltramadol
) and
SNRI
.
|
IM, IV, PO, rectal.
|
Bioavailability = 70?75% (oral), 100% (IM); protein binding = 20%; hepatic metabolism, via
CYP3A4
and
CYP2D6
; half-life = 6 hours; excretion = urine, faeces.
|
Moderate-severe pain.
|
As per other opioids but with less respiratory depression and constipation. Psychiatric AEs reported. Serotonin syndrome possible if used in conjunction with other serotonergics.
|
Anilidopiperidines
|
Alfentanil
|
Comes in hydrochloride salt form; freely soluble in ethanol, water, methanol; degrades upon contact with air and light.
|
Mu opioid.
|
Epidural, IM, IV, intrathecally.
|
Protein binding = 90%; volume of distribution = small; half-life = 1?2 hours; hepatic metabolism, mostly via
CYP3A4
; excretion = urine.
|
Procedural anaesthesia.
|
As per other opioids. Very sedating.
|
Fentanyl
|
Comes in free, hydrochloride salt, citrate salt forms; practically insoluble in water (free form), soluble in water (citrate salt form), freely soluble in ethanol and methanol; degrades outside the temperature range of 15 °C and 30 °C and upon contact with light.
|
Mu opioid.
|
Buccal, epidermal, IM, IV, intrathecal, intranasal, SC, sublingual.
|
Bioavailability = 50% (buccal), 89% (intranasal); protein binding = 80%; hepatic metabolism, mostly via
CYP3A4
; half-life = 219 min; excretion = urine (primary), faeces.
|
Moderate-severe pain (including labour pain); adjunct to anaesthesia.
|
As with other opioids, with less nausea, vomiting, constipation and itching and more sedation.
|
Remifentanil
|
Comes in hydrochloride salt.
|
Mu opioid.
|
IV.
|
Protein binding = 70%; hydrolysed by blood and tissue esterases; half-life = 20 min; excretion = urine (95%).
|
Anaesthesia maintenance.
|
As with fentanyl.
|
Sufentanil
|
Comes in free and citrate salt forms; soluble in water, ethanol and methanol; degrades upon contact with light and temperatures outside 15 °C and 30 °C.
|
Mu opioid.
|
Epidural, IV, intrathecal, transdermal.
|
Protein binding = 90%; half-life = 2.5 hours; excretion = urine (80%).
|
Adjunct to anaesthesia and moderate-severe pain.
|
As with fentanyl.
|
Other analgesics
|
Acetanilide
|
No data.
|
Paracetamol prodrug.
|
PO.
|
No data.
|
Pain; fever.
|
Cancer; AEs of paracetamol.
|
Amitriptyline
|
Comes in free form and in hydrochloride and embonate salt forms; practically insoluble in water (embonate salt), freely soluble in water (HCl); degrades upon contact with light.
|
SNRI.
|
PO.
|
Hepatic metabolism, via
CYP2C19
,
CYP3A4
; active metabolite, nortriptyline; half-life = 9?27 hours; excretion = urine (18%), faeces.
|
Neuropathic pain; nocturnal enuresis; major depression; migraine prophylaxis; urinary urge incontinence.
|
Sedation, anticholinergic effects, weight gain, orthostatic hypotension,
sinus tachycardia
, sexual dysfunction, tremor, dizziness, sweating, agitation, insomnia, anxiety, confusion.
|
Dronabinol
|
Comes in free form; degrades upon contact with light.
|
Cannabinoid receptor partial agonist.
|
PO.
|
Bioavailability = 10?20%; protein binding = 90?99%; volume of distribution = 10 L/kg; hepatic metabolism; half-life = 25?36 hours, 44?59 hours (metabolites); excretion = faeces (50%), urine (15%).
[119]
|
Refractory chemotherapy-induced nausea and vomiting; anorexia; neuropathic pain.
|
Dizziness, euphoria, paranoia, somnolence, abnormal thinking, abdominal pain, nausea, vomiting, depression, hallucinations, hypotension, special difficulties, emotional lability, tremors, flushing, etc.
|
Duloxetine
|
Comes in hydrochloride salt form; slightly soluble in water, freely soluble in methanol; degrades upon contact with light.
|
SNRI.
|
PO.
|
Protein binding > 90%; volume of distribution = 3.4 L/kg; hepatic metabolism, via
CYP2D6
,
CYP1A2
; half-life = 12 hours; excretion = urine (70%), faeces (20%).
[120]
|
Major depression; generalised anxiety disorder; neuropathic pain.
|
Anticholinergic effects, GI effects, yawning, sweating, dizziness, weakness, sexual dysfunction, somnolence, insomnia, headache, tremor, decreased appetite.
|
Flupirtine
|
Comes as maleate salt. Chemically related to
retigabine
.
|
Potassium channel (Kv7) opener.
[121]
|
PO, rectal.
|
Bioavailability = 90% (oral), 72.5% (rectal); protein binding = 80%; volume of distribution = 154 L; hepatic metabolism; half-life = 6.5 hours; excretion = urine (72%).
|
Pain;
fibromyalgia
;
Creutzfeldt?Jakob disease
.
|
Drowsiness, dizziness, heartburn, dry mouth, fatigue and nausea.
[122]
|
Gabapentin
|
Comes in free and enacarbil salt forms; fairly insoluble in ethanol, dichoromethane, fairly soluble in water.
|
Binds to the α2δ-1 subunit of voltage gated calcium ion channels in the spinal cord. May also modulate NMDA receptors and protein kinase C.
|
PO.
|
Half-life = 5?7 hours.
|
Neuropathic pain; epilepsy.
|
Fatigue, sedation, dizziness, ataxia, tremor, diplopia, nystagmus, amblyopia, amnesia, abnormal thinking, hypertension, vasodilation, peripheral oedema, dry mouth, weight gain and rash.
|
Milnacipran
|
No data.
|
SNRI.
|
PO.
|
Bioavailability = 85?90%; protein binding = 13%: volume of distribution = 400 L; hepatic metabolism; half-life = 6?8 hours (L-isomer), 8?10 hours (D-isomer); excretion = urine (55%).
[123]
|
Fibromyalgia
.
|
As per duloxetine, plus hypertension.
|
Nabiximols
|
Contains
cannabidiol
and
dronabinol
in roughly equal concentrations.
|
As per dronabinol.
|
Buccal spray.
|
Not available.
|
Neuropathic pain and spasticity as part of
MS
.
|
As per dronabinol.
|
Nefopam
|
Comes in a hydrochloride salt form. Chemically related to
orphenadrine
.
|
Unknown;
serotonin-norepinephrine-dopamine reuptake inhibitor
.
|
PO, IM.
|
Protein binding = 73%; half-life = 4 hours; excretion = urine, faeces (8%).
|
Analgesia, especially postoperative;
hiccups
.
|
Has antimuscarinic and sympathomimetic effects.
[124]
|
Paracetamol
|
Comes in free form; practically insoluble in water, freely soluble in ethanol; degrades upon contact with moisture, air and light.
|
Multiple; inhibits prostaglandin synthesis in the CNS, an active metabolite,
AM404
, is an
anandamide
reuptake inhibitor.
|
PO, IV, IM, rectal.
|
Protein binding = 10?25%; volume of distribution = 1 L/kg; hepatic metabolism; half-life = 1?3 hours; excretion = urine.
[125]
|
Analgesia and fever reduction.
|
Hepatotoxicity; hypersensitivity reactions (rare), including
Stevens?Johnson syndrome
; hypotension (rare; IV).
|
Phenacetin
|
No data.
|
Prodrug to paracetamol.
|
PO.
|
No data.
|
Analgesia and fever reduction.
|
Haematologic, nephrotoxicity, cancer and paracetamol AEs.
|
Pregabalin
|
Comes in free form.
|
As per gabapentin.
|
PO.
|
Bioavailability = 90%; half-life = 6.3 hours; hepatic metabolism; excretion = urine (90%).
[126]
|
Neuropathic pain; anxiety; epilepsy.
|
As per gabapentin.
|
Propacetamol
|
Freely soluble in water; degrades upon contact with moisture.
|
Prodrug to paracetamol.
|
IM, IV.
|
No data available.
|
Analgesia and fever reduction.
|
As per paracetamol.
|
Ziconotide
|
Peptide.
|
N-type calcium-channel blocker.
|
Intrathecal.
|
Protein binding = 50%; half-life = 2.9?6.5 hours; excretion = urine (<1%).
[127]
|
Chronic pain.
|
CNS toxicity (abnormal gait, abnormal vision, memory problems, etc.); GI effects.
[127]
|
Where † indicates products that are no longer marketed.
|