Dosing & Uses
Dosage Forms & Strengths
powder for injection
- 5mg
injectable solution
- 0.4mg/1.7mL
Pheochromocytoma
Diagnosis: 5 mg IV/IM
Test for pheochromocytoma is positive if decrease SBP >35 mmHg & decrease DBP >25 mmHg
Pheochromocytoma Surgery Use
Treatment of hypertension during pheochromocytoma surgery
5 mg IV/IM 1-2 hr preoperative, repeat if necessary q2-4hr
Extravasation Treatment
Epinephrine or norepinephrine extravastation treatment
Treatment: 5-10 mg in 10 mL NS local injection within 12 hr
Prevention: 10 mg for each liter of IV fluids (pressor effect of NE is unaffected)
Dental Anesthesia Reversal (OraVerse)
Indicated for reversal of soft-tissue anesthesia associated with functional deficits from intraoral local anesthesia containing a vasoconstrictor
Dose based on amount of local anesthetic administered
Administer using same locations and techniques (infiltration or block injection) as local anesthetic
1/2 cartridge local anesthetic: OraVerse 1/2 cartridge (0.2 mg)
1 cartridge local anesthetic: OraVerse 1 cartridge (0.4 mg)
2 cartridges local anesthetic: OraVerse 2 cartridges (0.8 mg)
Hypertensive Crises (Off-label)
Secondary to catecholamine excess: 5-15 mg IV
Other Indications & Uses
Pheochromocytoma diagnosis, HTN in pheochromocytoma surgery, dermal necrosis due to epinephrine/NE extravasation
Off-label: hypertensive crises (pheochromocytoma, other catecholamine excess situations); erectile dysfunction (intracavernous)
Dosage Forms & Strengths
powder for injection
- 5mg
injectable solution
- 0.4mg/1.7mL
Pheochromocytoma, Diagnosis
0.1-0.2 mg/kg IV/IM, OR 1 mg IV OR 3 mg IM
Pheochromocytoma Surgery Use
Treatment of hypertension during surgery
0.05-0.1 mg/kg/dose OR 1 mg IV/IM 1-2 hr preoperative, repeat q2-4hr until hypertension is controlled; not to exceed 5 mg/dose
Dental Anesthesia Reversal (OraVerse)
Indicated for reversal of soft-tissue anesthesia associated with functional deficits from intraoral local anesthesia containing a vasoconstrictor
<6 years or <15 kg: Safety and efficacy not established
Dose based on amount of local anesthetic administered
Administer using same locations and techniques (infiltration or block injection) as local anesthetic
6-12 years (15-30 kg)
- For 1/2 cartridge local anesthetic, use OraVerse 1/2 cartridge (0.2 mg)
6-12 years (>30 kg)
- 1/2 cartridge local anesthetic: OraVerse 1/2 cartridge (0.2 mg)
- 1 cartridge local anesthetic: OraVerse 1 cartridge (0.4 mg)
Other Information
Extravasation of epinephrine/norepinephrine:0.1-0.2 mg/kg to no more than 10 mg
Pheochromocytoma
Diagnosis: 5 mg IV/IM
Test for pheochromocytoma is positive if decrease SBP >35 mmHg & decrease DBP >25 mmHg
Pheochromocytoma surgery use
Treatment of hypertension during pheochromocytoma surgery
5 mg IV/IM 1-2 hr preoperative, repeat if necessary q2-4hr
Extravasation treatment
Epinephrine or norepinephrine extravastation treatment
Treatment: 5-10 mg in 10 mL NS local injection within 12 hr
Prevention: 10 mg for each liter of IV fluids (pressor effect of NE is unaffected)
Dental anesthesia reversal (OraVerse)
Indicated for reversal of soft-tissue anesthesia associated with functional deficits from intraoral local anesthesia containing a vasoconstrictor
Dose based on amount of local anesthetic administered
Administer using same locations and techniques (infiltration or block injection) as local anesthetic
1/2 cartridge local anesthetic: OraVerse 1/2 cartridge (0.2 mg)
1 cartridge local anesthetic: OraVerse 1 cartridge (0.4 mg)
2 cartridges local anesthetic: OraVerse 2 cartridges (0.8 mg)
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Contraindicated (0)
Serious - Use Alternative (5)
- lofexidine
lofexidine, phentolamine. Either increases effects of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid coadministration with other drugs that decrease pulse or blood pressure to mitigate risk of excessive bradycardia and hypotension.
- sildenafil
sildenafil increases effects of phentolamine by pharmacodynamic synergism. Avoid or Use Alternate Drug. Risk of hypotension; separate sildenafil >25mg from alpha blocker by 4hr.
- tamsulosin
phentolamine, tamsulosin. Either increases effects of the other by additive vasodilation. Avoid or Use Alternate Drug. Risk of hypotension.
- vardenafil
vardenafil increases effects of phentolamine by pharmacodynamic synergism. Contraindicated. Risk of hypotension.
- yohimbe
yohimbe increases effects of phentolamine by pharmacodynamic synergism. Contraindicated.
Monitor Closely (93)
- acebutolol
phentolamine and acebutolol both increase anti-hypertensive channel blocking. Modify Therapy/Monitor Closely.
- aceclofenac
aceclofenac decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- acemetacin
acemetacin decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- aldesleukin
aldesleukin increases effects of phentolamine by pharmacodynamic synergism. Use Caution/Monitor. Risk of hypotension.
- alfuzosin
alfuzosin and phentolamine both increase anti-hypertensive channel blocking. Use Caution/Monitor.
- amifostine
amifostine, phentolamine. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Coadministration with blood pressure lowering agents may increase the risk and severity of hypotension associated with amifostine. When amifostine is used at chemotherapeutic doses, withhold blood pressure lowering medications for 24 hr prior to amifostine; if blood pressure lowering medication cannot be withheld, do not administer amifostine.
- amlodipine
phentolamine and amlodipine both increase anti-hypertensive channel blocking. Use Caution/Monitor.
- asenapine
asenapine and phentolamine both increase anti-hypertensive channel blocking. Use Caution/Monitor.
- aspirin
aspirin decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- aspirin rectal
aspirin rectal decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- aspirin/citric acid/sodium bicarbonate
aspirin/citric acid/sodium bicarbonate decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- atenolol
phentolamine and atenolol both increase anti-hypertensive channel blocking. Modify Therapy/Monitor Closely.
- avanafil
avanafil increases effects of phentolamine by pharmacodynamic synergism. Use Caution/Monitor. Risk of hypotension.
- benazepril
benazepril, phentolamine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Exaggerated first dose hypotensive response.
- betaxolol
phentolamine and betaxolol both increase anti-hypertensive channel blocking. Modify Therapy/Monitor Closely.
- bisoprolol
phentolamine and bisoprolol both increase anti-hypertensive channel blocking. Modify Therapy/Monitor Closely.
- bretylium
phentolamine, bretylium. Either increases effects of the other by pharmacodynamic synergism. Modify Therapy/Monitor Closely. Each drug may cause hypotension.
- captopril
captopril, phentolamine. Either increases effects of the other by Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Exaggerated first dose hypotensive response. Both drugs lower blood pressure. Monitor blood pressure.
- carbidopa
carbidopa increases effects of phentolamine by pharmacodynamic synergism. Use Caution/Monitor. Monitor for hypotension.
- carvedilol
phentolamine and carvedilol both increase anti-hypertensive channel blocking. Modify Therapy/Monitor Closely.
- celecoxib
celecoxib decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- celiprolol
phentolamine and celiprolol both increase anti-hypertensive channel blocking. Modify Therapy/Monitor Closely.
- choline magnesium trisalicylate
choline magnesium trisalicylate decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- clevidipine
phentolamine and clevidipine both increase anti-hypertensive channel blocking. Use Caution/Monitor.
- diclofenac
diclofenac decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- diflunisal
diflunisal decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- diltiazem
phentolamine and diltiazem both increase anti-hypertensive channel blocking. Use Caution/Monitor.
- dopexamine
phentolamine, dopexamine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Hypotension, tachycardia.
- doxazosin
doxazosin and phentolamine both increase anti-hypertensive channel blocking. Use Caution/Monitor.
- enalapril
enalapril, phentolamine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Exaggerated first dose hypotensive response.
- ephedrine
phentolamine, ephedrine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Hypotension, tachycardia.
- epinephrine
phentolamine, epinephrine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Hypotension, tachycardia.
- epinephrine racemic
phentolamine, epinephrine racemic. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Hypotension, tachycardia.
- esmolol
phentolamine and esmolol both increase anti-hypertensive channel blocking. Modify Therapy/Monitor Closely.
- etodolac
etodolac decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- felodipine
phentolamine and felodipine both increase anti-hypertensive channel blocking. Use Caution/Monitor.
- fenoprofen
fenoprofen decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- flurbiprofen
flurbiprofen decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- fosinopril
fosinopril, phentolamine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Exaggerated first dose hypotensive response.
- ibuprofen
ibuprofen decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- ibuprofen IV
ibuprofen IV decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- iloperidone
iloperidone increases effects of phentolamine by pharmacodynamic synergism. Use Caution/Monitor.
- imidapril
imidapril, phentolamine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Exaggerated first dose hypotensive response.
- indomethacin
indomethacin decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- isradipine
phentolamine and isradipine both increase anti-hypertensive channel blocking. Use Caution/Monitor.
- ketoprofen
ketoprofen decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- ketorolac
ketorolac decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- ketorolac intranasal
ketorolac intranasal decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- labetalol
phentolamine and labetalol both increase anti-hypertensive channel blocking. Modify Therapy/Monitor Closely.
- levodopa
levodopa increases effects of phentolamine by pharmacodynamic synergism. Use Caution/Monitor. Consider decreasing dosage of antihypertensive agent.
- lisinopril
lisinopril, phentolamine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Exaggerated first dose hypotensive response.
- lornoxicam
lornoxicam decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- meclofenamate
meclofenamate decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- mefenamic acid
mefenamic acid decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- meloxicam
meloxicam decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- methylphenidate
methylphenidate will decrease the level or effect of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. Methylphenidate may diminish antihypertensive effects. Monitor BP.
- metoprolol
phentolamine and metoprolol both increase anti-hypertensive channel blocking. Modify Therapy/Monitor Closely.
- moexipril
moexipril, phentolamine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Exaggerated first dose hypotensive response.
- moxisylyte
moxisylyte and phentolamine both increase anti-hypertensive channel blocking. Use Caution/Monitor.
- nabumetone
nabumetone decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- nadolol
phentolamine and nadolol both increase anti-hypertensive channel blocking. Modify Therapy/Monitor Closely.
- naproxen
naproxen decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- nebivolol
phentolamine and nebivolol both increase anti-hypertensive channel blocking. Modify Therapy/Monitor Closely.
- nicardipine
phentolamine and nicardipine both increase anti-hypertensive channel blocking. Use Caution/Monitor.
- nifedipine
phentolamine and nifedipine both increase anti-hypertensive channel blocking. Use Caution/Monitor.
- nisoldipine
phentolamine and nisoldipine both increase anti-hypertensive channel blocking. Use Caution/Monitor.
- norepinephrine
phentolamine, norepinephrine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Hypotension, tachycardia.
- oxaprozin
oxaprozin decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- oxymetazoline topical
oxymetazoline topical increases and phentolamine decreases sympathetic (adrenergic) effects, including increased blood pressure and heart rate. Effect of interaction is not clear, use caution. Use Caution/Monitor.
- parecoxib
parecoxib decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- penbutolol
phentolamine and penbutolol both increase anti-hypertensive channel blocking. Modify Therapy/Monitor Closely.
- perindopril
perindopril, phentolamine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Exaggerated first dose hypotensive response.
- phenoxybenzamine
phenoxybenzamine and phentolamine both increase anti-hypertensive channel blocking. Use Caution/Monitor.
- pindolol
phentolamine and pindolol both increase anti-hypertensive channel blocking. Modify Therapy/Monitor Closely.
- piroxicam
piroxicam decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- prazosin
phentolamine and prazosin both increase anti-hypertensive channel blocking. Use Caution/Monitor.
- propranolol
phentolamine and propranolol both increase anti-hypertensive channel blocking. Modify Therapy/Monitor Closely.
- quinapril
quinapril, phentolamine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Exaggerated first dose hypotensive response.
- ramipril
ramipril, phentolamine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Exaggerated first dose hypotensive response.
- salicylates (non-asa)
salicylates (non-asa) decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- salsalate
salsalate decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- silodosin
phentolamine and silodosin both increase anti-hypertensive channel blocking. Use Caution/Monitor.
- sotalol
phentolamine and sotalol both increase anti-hypertensive channel blocking. Modify Therapy/Monitor Closely.
- sulfasalazine
sulfasalazine decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- sulindac
sulindac decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- tadalafil
tadalafil increases effects of phentolamine by pharmacodynamic synergism. Use Caution/Monitor. Risk of hypotension.
- terazosin
phentolamine and terazosin both increase anti-hypertensive channel blocking. Use Caution/Monitor.
- timolol
phentolamine and timolol both increase anti-hypertensive channel blocking. Modify Therapy/Monitor Closely.
- tolfenamic acid
tolfenamic acid decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- tolmetin
tolmetin decreases effects of phentolamine by pharmacodynamic antagonism. Use Caution/Monitor. NSAIDs decrease prostaglandin synthesis.
- trandolapril
trandolapril, phentolamine. Mechanism: pharmacodynamic synergism. Use Caution/Monitor. Exaggerated first dose hypotensive response.
- verapamil
phentolamine and verapamil both increase anti-hypertensive channel blocking. Use Caution/Monitor.
- zotepine
phentolamine and zotepine both increase anti-hypertensive channel blocking. Use Caution/Monitor.
Minor (7)
- brimonidine
brimonidine increases effects of phentolamine by pharmacodynamic synergism. Minor/Significance Unknown.
- butcher's broom
phentolamine, butcher's broom. Either decreases effects of the other by Mechanism: pharmacodynamic antagonism. Minor/Significance Unknown.
- ethanol
phentolamine, ethanol. Mechanism: pharmacodynamic synergism. Minor/Significance Unknown. Risk of hypotension, esp. in Asian pts.
- phenylephrine
phentolamine, phenylephrine. Either decreases effects of the other by Mechanism: pharmacodynamic antagonism. Minor/Significance Unknown.
- phenylephrine PO
phentolamine, phenylephrine PO. Either decreases effects of the other by Mechanism: pharmacodynamic antagonism. Minor/Significance Unknown.
- tizanidine
tizanidine increases effects of phentolamine by pharmacodynamic synergism. Minor/Significance Unknown. Risk of hypotension.
- treprostinil
treprostinil increases effects of phentolamine by pharmacodynamic synergism. Minor/Significance Unknown.
Adverse Effects
1-10%
Nasal congestion (10% )
Post-treatment pain (up to 10% )
Injection site pain (4% to 6% )
Diarrhea (<3% )
Frequency Not Defined
Cardiac dysrhythmia
Chest pain
Hypotension
Myocardial infarction
CVA - cerebrovascular accident due to cerebral artery occlusion
Warnings
Contraindications
Hypersensitivity; MI or other CAD
Cautions
First dose effect may occur, causing a sudden and drastic fall in blood pressure after administering the first dose.
Hypotension/syncope with first few doses or with increase in dose; minimize by using small first dose at bedtime
Increase dose slowly
Myocardial infarction, cerebrovascular spasm, and cerebrovascular occlusion reported following parenteral administration of phentolamine; these events usually occurred in association with marked hypotensive episodes producing shock-like states
Tachycardia and cardiac arrhythmias may occur with use of phentolamine or other alpha-adrenergic blocking agents; although such effects are uncommon after administration, clinicians should be alert to signs and symptoms of these events, particularly in patients with a prior history of cardiovascular disease; discontinue if angina occur or worsen
Pregnancy & Lactation
Pregnancy Category: C
Lactation: not known if excreted in breast milk; not recommended
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Has positive inotropic and chronotropic effect on the heart
Blocks alph-adrenergic receptors to briefly antagonize circulating epinephrine and norepinephrine to reduce hypertension caused by alpha effects of the endogenous catecholamines
Pharmacokinetics
Half-Life:19 min (IV)
Duration: 30-45 min (IM); 15-30 min (IV)
Excretion: Urine (13%) as unchanged drug
Metabolism: Hepatic
Onset of action: Immediate (IV); 15-20 min (IM)
Peak effect: 10-20 min (OraVerse)
Administration
IV Compatibilities
Additive: cibenzoline succinate, dobutamine, verapamil
Syringe: papaverine
Y-site: amiodarone
IV Preparation
Reconstitute with 1 mL SWI (5 mg/mL solution)
IV/IM Administration
Administer by IV or IM injection
Rapid IV
Storage
Store at controlled room temperature
Images
BRAND | FORM. | UNIT PRICE | PILL IMAGE |
---|---|---|---|
phentolamine injection - | 5 mg vial | ![]() | |
phentolamine injection - | 5 mg vial | ![]() | |
phentolamine injection - | 5 mg vial | ![]() | |
phentolamine injection - | 5 mg vial | ![]() |
Copyright © 2010 First DataBank, Inc.
Patient Handout
phentolamine injection
NO MONOGRAPH AVAILABLE AT THIS TIME
USES: Consult your pharmacist.
HOW TO USE: Consult your pharmacist.
SIDE EFFECTS: Consult your pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Consult your pharmacist.
DRUG INTERACTIONS: Consult your pharmacist.Keep a list of all your medications with you, and share the list with your doctor and pharmacist.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: No monograph available at this time.
MISSED DOSE: Consult your pharmacist.
STORAGE: Consult your pharmacist.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.
Information last revised July 2016. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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