Tapentadol

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

  1. adrenocortical insufficiency
  2. agitation
  3. amenorrhea
  4. anaphylactic shock
  5. anaphylactoid reactions
  6. angioedema
  7. anorexia
  8. anxiety
  9. asthenia
  10. blurred vision
  11. bradycardia
  12. bundle-branch block
  13. chills
  14. confusion
  15. constipation
  16. cough
  17. depression
  18. diarrhea
  19. dizziness
  20. drowsiness
  21. dysarthria
  22. dyspepsia
  23. dysphoria
  24. dyspnea
  25. euphoria
  26. fatigue
  27. flushing
  28. gonadal suppression
  29. hallucinations
  30. headache
  31. hyperhidrosis
  32. hypoesthesia
  33. hyponatremia
  34. hypotension
  35. hypoxia
  36. impaired cognition
  37. impotence (erectile dysfunction)
  38. increased urinary frequency
  39. infection
  40. infertility
  41. insomnia
  42. irritability
  43. lethargy
  44. libido decrease
  45. memory impairment
  46. nausea
  47. neonatal opioid withdrawal syndrome
  48. orthostatic hypotension
  49. palpitations
  50. paresthesias
  51. pharyngitis
  52. physiological dependence
  53. pruritus
  54. psychological dependence
  55. psychomotor impairment
  56. rash
  57. respiratory depression
  58. restlessness
  59. seizures
  60. serotonin syndrome
  61. SIADH
  62. sinus tachycardia
  63. suicidal ideation
  64. syncope
  65. tolerance
  66. tremor
  67. urinary retention
  68. urticaria
  69. vertigo
  70. vomiting
  71. weight loss
  72. withdrawal
  73. 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
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