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