What is Tapentadol
Tapentadol is an oral opioid agonist indicated for severe pain.
It activates the mu-opioid receptor and inhibits norepinephrine synaptic reuptake. Norepinephrine reuptake inhibition appears to have additive analgesic effect to that of the drug’s opioid activity.
Because no metabolic activation appears to be necessary for analgesia and no active metabolites have been identified, tapentadol may be a preferred analgesic in patients with altered cytochrome P450 (CYP450) activity or in those with mild hepatic or mild to moderate renal impairment; use is not recommended in patients with severe hepatic or renal dysfunction.
Immediate-release tapentadol was similarly effective in treating chronic pain and postsurgical acute pain when compared to oral immediate-release oxycodone and morphine in clinical trials.
Brand Name
Nucynta |
Nucynta ER
Indications
- neuropathic pain
- severe pain
Side Effects
- adrenocortical insufficiency
- agitation
- amenorrhea
- anaphylactic shock
- anaphylactoid reactions
- angioedema
- anorexia
- anxiety
- asthenia
- blurred vision
- bradycardia
- bundle-branch block
- chills
- confusion
- constipation
- cough
- depression
- diarrhea
- dizziness
- drowsiness
- dysarthria
- dyspepsia
- dysphoria
- dyspnea
- euphoria
- fatigue
- flushing
- gonadal suppression
- hallucinations
- headache
- hyperhidrosis
- hypoesthesia
- hyponatremia
- hypotension
- hypoxia
- impaired cognition
- impotence (erectile dysfunction)
- increased urinary frequency
- infection
- infertility
- insomnia
- irritability
- lethargy
- libido decrease
- memory impairment
- nausea
- neonatal opioid withdrawal syndrome
- orthostatic hypotension
- palpitations
- paresthesias
- pharyngitis
- physiological dependence
- pruritus
- psychological dependence
- psychomotor impairment
- rash
- respiratory depression
- restlessness
- seizures
- serotonin syndrome
- SIADH
- sinus tachycardia
- suicidal ideation
- syncope
- tolerance
- tremor
- urinary retention
- urticaria
- vertigo
- vomiting
- weight loss
- withdrawal
- xerostomia
Monitoring Parameters
- laboratory monitoring not necessary
- neurologic function
Contraindications
- abrupt discontinuation
- accidental exposure
- acute abdomen
- adrenal insufficiency
- alcoholism
- angina
- asthma
- biliary tract disease
- bladder obstruction
- breast-feeding
- cardiac arrhythmias
- cardiac disease
- children
- chronic obstructive pulmonary disease (COPD)
- CNS depression
- coadministration with other CNS depressants
- coma
- constipation
- cor pulmonale
- dehydration
- depression
- diarrhea
- driving or operating machinery
- ethanol ingestion
- ethanol intoxication
- geriatric
- GI disease
- GI obstruction
- head trauma
- heart failure
- hepatic disease
- hypotension
- hypothyroidism
- hypovolemia
- hypoxemia
- ileus
- increased intracranial pressure
- infants
- infertility
- inflammatory bowel disease
- intracranial mass
- labor
- MAOI therapy
- myxedema
- neonatal opioid withdrawal syndrome
- neonates
- obesity
- obstetric delivery
- oliguria
- opioid-naive patients
- orthostatic hypotension
- pancreatitis
- parenteral administration
- potential for overdose or poisoning
- pregnancy
- prostatic hypertrophy
- psychosis
- pulmonary disease
- renal failure
- renal impairment
- reproductive risk
- requires an experienced clinician
- respiratory depression
- respiratory insufficiency
- scoliosis
- seizure disorder
- seizures
- shock
- sleep apnea
- status asthmaticus
- substance abuse
- ulcerative colitis
- urethral stricture
- urinary retention
Interactions
- AbobotulinumtoxinA
- Acetaminophen; Butalbital
- Acetaminophen; Butalbital; Caffeine
- Acetaminophen; Butalbital; Caffeine; Codeine
- Acetaminophen; Caffeine; Dihydrocodeine
- Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
- Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
- Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
- Acetaminophen; Codeine
- Acetaminophen; Dextromethorphan; Doxylamine
- Acetaminophen; Dichloralphenazone; Isometheptene
- Acetaminophen; Diphenhydramine
- Acetaminophen; Hydrocodone
- Acetaminophen; Oxycodone
- Acetaminophen; Propoxyphene
- Acetaminophen; Tramadol
- Alfentanil
- Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
- Aliskiren; Hydrochlorothiazide, HCTZ
- Alprazolam
- Amifampridine
- Amiloride
- Amiloride; Hydrochlorothiazide, HCTZ
- Amitriptyline
- Amitriptyline; Chlordiazepoxide
- Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
- Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
- Amobarbital
- Amoxapine
- Anticholinergics
- Antidiarrheals
- Anxiolytics; Sedatives; and Hypnotics
- Apomorphine
- Aripiprazole
- Asenapine
- Aspirin, ASA; Butalbital; Caffeine
- Aspirin, ASA; Butalbital; Caffeine; Codeine
- Aspirin, ASA; Caffeine; Dihydrocodeine
- Aspirin, ASA; Carisoprodol; Codeine
- Aspirin, ASA; Oxycodone
- Atazanavir
- Atazanavir; Cobicistat
- Atenolol; Chlorthalidone
- Atomoxetine
- Atracurium
- Atropine
- Atropine; Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
- Atropine; Difenoxin
- Atropine; Diphenoxylate
- Atropine; Edrophonium
- Atropine; Hyoscyamine; Phenobarbital; Scopolamine
- Azelastine
- Azelastine; Fluticasone
- Azilsartan; Chlorthalidone
- Barbiturates
- Belladonna Alkaloids; Ergotamine; Phenobarbital
- Belladonna; Opium
- Benazepril; Hydrochlorothiazide, HCTZ
- Bendroflumethiazide; Nadolol
- Benzhydrocodone; Acetaminophen
- Benzoic Acid; Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate
- Benztropine
- Bisoprolol; Hydrochlorothiazide, HCTZ
- Botulinum Toxins
- Brexpiprazole
- Brompheniramine
- Brompheniramine; Carbetapentane; Phenylephrine
- Brompheniramine; Dextromethorphan; Guaifenesin
- Brompheniramine; Guaifenesin; Hydrocodone
- Brompheniramine; Hydrocodone; Pseudoephedrine
- Brompheniramine; Pseudoephedrine
- Bumetanide
- Buprenorphine; Naloxone
- Bupropion; Naltrexone
- Buspirone
- Butabarbital
- Candesartan; Hydrochlorothiazide, HCTZ
- Cannabidiol
- Captopril; Hydrochlorothiazide, HCTZ
- Carbetapentane; Chlorpheniramine
- Carbetapentane; Chlorpheniramine; Phenylephrine
- Carbetapentane; Diphenhydramine; Phenylephrine
- Carbidopa; Levodopa; Entacapone
- Carbinoxamine; Hydrocodone; Phenylephrine
- Carbinoxamine; Hydrocodone; Pseudoephedrine
- Cenobamate
- Cetirizine
- Cetirizine; Pseudoephedrine
- Chloral Hydrate
- Chlordiazepoxide
- Chlordiazepoxide; Clidinium
- Chlorothiazide
- Chlorpheniramine
- Chlorpheniramine; Codeine
- Chlorpheniramine; Dextromethorphan
- Chlorpheniramine; Dextromethorphan; Phenylephrine
- Chlorpheniramine; Dihydrocodeine; Phenylephrine
- Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
- Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
- Chlorpheniramine; Hydrocodone
- Chlorpheniramine; Hydrocodone; Phenylephrine
- Chlorpheniramine; Hydrocodone; Pseudoephedrine
- Chlorpheniramine; Phenylephrine
- Chlorpheniramine; Pseudoephedrine
- Chlorpromazine
- Chlorthalidone
- Chlorthalidone; Clonidine
- Cisatracurium
- Citalopram
- Clemastine
- Clobazam
- Clomipramine
- Clonazepam
- Clopidogrel
- Clorazepate
- Clozapine
- Codeine
- Codeine; Guaifenesin
- Codeine; Phenylephrine; Promethazine
- Codeine; Promethazine
- COMT inhibitors
- Cyproheptadine
- Darifenacin
- Desipramine
- Deutetrabenazine
- Dextromethorphan; Diphenhydramine; Phenylephrine
- Dextromethorphan; Promethazine
- Diazepam
- Dicyclomine
- Dihydrocodeine; Guaifenesin; Pseudoephedrine
- Dimenhydrinate
- Diphenhydramine
- Diphenhydramine; Hydrocodone; Phenylephrine
- Diphenhydramine; Ibuprofen
- Diphenhydramine; Naproxen
- Diphenhydramine; Phenylephrine
- Dolasetron
- Doxacurium
- Doxepin
- Doxylamine
- Doxylamine; Pyridoxine
- Dronabinol
- Droperidol
- Enalapril; Hydrochlorothiazide, HCTZ
- Enflurane
- Entacapone
- Eprosartan; Hydrochlorothiazide, HCTZ
- Escitalopram
- Esketamine
- Estazolam
- Eszopiclone
- Ethacrynic Acid
- Ethanol
- Etomidate
- Fentanyl
- Flavoxate
- Fluoxetine
- Fluoxetine; Olanzapine
- Fluphenazine
- Flurazepam
- Fluvoxamine
- Fosinopril; Hydrochlorothiazide, HCTZ
- Fospropofol
- Furosemide
- Gabapentin
- General anesthetics
- Glycopyrrolate
- Glycopyrrolate; Formoterol
- Granisetron
- Guaifenesin; Hydrocodone
- Guaifenesin; Hydrocodone; Pseudoephedrine
- Haloperidol
- Halothane
- Homatropine; Hydrocodone
- Hydralazine; Hydrochlorothiazide, HCTZ
- Hydrochlorothiazide, HCTZ
- Hydrochlorothiazide, HCTZ; Irbesartan
- Hydrochlorothiazide, HCTZ; Lisinopril
- Hydrochlorothiazide, HCTZ; Losartan
- Hydrochlorothiazide, HCTZ; Methyldopa
- Hydrochlorothiazide, HCTZ; Metoprolol
- Hydrochlorothiazide, HCTZ; Moexipril
- Hydrochlorothiazide, HCTZ; Olmesartan
- Hydrochlorothiazide, HCTZ; Propranolol
- Hydrochlorothiazide, HCTZ; Quinapril
- Hydrochlorothiazide, HCTZ; Spironolactone
- Hydrochlorothiazide, HCTZ; Telmisartan
- Hydrochlorothiazide, HCTZ; Triamterene
- Hydrochlorothiazide, HCTZ; Valsartan
- Hydrocodone
- Hydrocodone; Ibuprofen
- Hydrocodone; Phenylephrine
- Hydrocodone; Potassium Guaiacolsulfonate
- Hydrocodone; Potassium Guaiacolsulfonate; Pseudoephedrine
- Hydrocodone; Pseudoephedrine
- Hydromorphone
- Hydroxyzine
- Hyoscyamine
- Hyoscyamine; Methenamine; Methylene Blue; Phenyl Salicylate; Sodium Biphosphate
- Ibuprofen; Oxycodone
- Imipramine
- IncobotulinumtoxinA
- Indacaterol; Glycopyrrolate
- Indapamide
- Isocarboxazid
- Isoflurane
- Ketamine
- Lasmiditan
- Lemborexant
- Levocetirizine
- Levorphanol
- Linezolid
- Lithium
- Lofexidine
- Loop diuretics
- Lorazepam
- Lumateperone
- Maprotiline
- Melatonin
- Mepenzolate
- Meperidine
- Meperidine; Promethazine
- Mephobarbital
- Meprobamate
- Methadone
- Methenamine; Sodium Acid Phosphate; Methylene Blue; Hyoscyamine
- Methocarbamol
- Methohexital
- Methscopolamine
- Methyclothiazide
- Methylene Blue
- Metoclopramide
- Metolazone
- Midazolam
- Mirtazapine
- Mivacurium
- Molindone
- Monoamine oxidase inhibitors
- Morphine
- Morphine; Naltrexone
- Nabilone
- Naloxone
- Naltrexone
- Nefazodone
- Neuromuscular blockers
- Nortriptyline
- Olanzapine
- OnabotulinumtoxinA
- Ondansetron
- Opiate Agonists
- Opiate Agonists-Antagonists
- Oxazepam
- Oxybutynin
- Oxycodone
- Oxymorphone
- Ozanimod
- Palonosetron
- Pancuronium
- Paroxetine
- Pentazocine; Naloxone
- Pentobarbital
- Perampanel
- Perphenazine
- Perphenazine; Amitriptyline
- Phenelzine
- Phenobarbital
- Phenylephrine; Promethazine
- Pimozide
- Potassium-sparing diuretics
- Pramipexole
- Prasugrel
- Pregabalin
- Primidone
- Procarbazine
- Prochlorperazine
- Promethazine
- Propantheline
- Propofol
- Propoxyphene
- Protriptyline
- Quazepam
- Quetiapine
- Ramelteon
- Rapacuronium
- Rasagiline
- Remifentanil
- RimabotulinumtoxinB
- Risperidone
- Rocuronium
- Ropinirole
- Rotigotine
- Safinamide
- Scopolamine
- Secobarbital
- Selective norepinephrine reuptake inhibitors
- Selective serotonin reuptake inhibitors
- Selegiline
- Serotonin norepinephrine reuptake inhibitors
- Serotonin-Receptor Agonists
- Serotonin-Receptor Antagonists
- Sertraline
- Sevoflurane
- Skeletal Muscle Relaxants
- Solifenacin
- Spironolactone
- Succinylcholine
- Sufentanil
- Suvorexant
- Tasimelteon
- Tedizolid
- Temazepam
- Thiazide diuretics
- Thiopental
- Thioridazine
- Ticagrelor
- Tizanidine
- Tolcapone
- Tolterodine
- Torsemide
- Tramadol
- Tranylcypromine
- Trazodone
- Triamterene
- Triazolam
- Tricyclic antidepressants
- Trifluoperazine
- Trihexyphenidyl
- Trimipramine
- Trospium
- Tubocurarine
- Valerian, Valeriana officinalis
- Valproic Acid, Divalproex Sodium
- Vecuronium
- Vilazodone
- Vortioxetine
- Zaleplon
- Ziprasidone
- Zolpidem