Clonidine Withdrawal

Published 2016-10-15 00:31:00 clonidine

Clonidine withdrawal is a serious matter. I've personally used clonidine to control high blood pressure. Physicians also prescribe clonidine to treat ADHD, though it's less popular for this purpose than psychostimulants.

Clonidine withdrawal can be managed by gradually tapering your dose and avoiding abrupt discontinuation. It's safest to discontinue clonidine under the guidance of your physician.

How Long Does Clonidine Withdrawal Last?

Take a look at Clonidine's half-life.

The half-life is the amount of time it takes for your body to clear 50% of a drug.

Clonidine pharmacokinetics

From the chart above, clondine concentrations peak after about 6 hours. Then clondine blood levels gradually taper to 50 ng/mL at the 48 hour mark. The half-life of clonidine is 14 hours +/- 2 hours. This means that after ~14 hour, 50% of your original dose of clonidine remains in your bloodstream, then after a total of ~28 hours, 25% remains, and so on.

Clonidine withdrawal symptoms last 1-2 weeks after stopping the drug. They are most severe around the 72 hour mark, after which you'll see gradually improvement in clonidine withdrawal symptoms.

Clonidine lowers blood pressure by suppressing norepinephrine activity. So when

How To Taper Clonidine

How can you safely wean off of clonidine?

You can reduce the dose by 25% or 1/4 each week as follows. More aggressive tapering schedules are not necessarily dangerous, but they will intensify clonidine withdrawl effects.

Starting Dose Week 1 Week 2 Week 3 Week 4
0.2 mg 0.15 mg 0.10 mg 0.05 mg 0

Research On Clonidine Withdrawal

There's some interesting stuff in the biomedical literature about clonidine withdrawal. For example, here's the abstract for one paper entitled Clonidine Withdrawal: Mechanism and Frequency of Rebound Hypertension1:

  1. The frequency and pathophysiology of the clonidine withdrawal syndrome was studied in fourteen hypertensive patients on chronic clonidine therapy.

  2. After sudden cessation of clonidine (900 jg daily) almost all of the patients showed an excessive increase of the heart rate and blood pressure. Seven of the fourteen patients had subjective symptoms, in three severe enough to require interruption of observation by therapeutic intervention 12 to 60 h after the last dose of clonidine. After clonidine withdrawal, NAE increased to abnormally high values in correlation with the blood pressure (P < 0.01) and heart rate (P < 0.00 1), whereas PRA even decreased initially, probably secondary to the rise of the blood pressure, and only rose, although not significantly, 48 h after withdrawal. PRA was not correlated with NAE, heart rate, or blood pressure.

  3. It is concluded that the clonidine withdrawal phenomenon is a frequently occurring and potentially dangerous syndrome. Overactivity of the sympathetic nervous system is mainly responsible, without the mediation of the renin angiotensin system. This also explains our experience that adrenergic preceptor blocking drugs do not prevent the rise in BP, although they alleviate some of the symptoms.

Clonidine Withdrawal Symptom

The most common and severe withdrawal symptoms of clonidine include: - Increased heartbeat - High blood pressure - Abnormal heartbeat

Other symptoms include:

  • Low blood pressure while standing
  • Nervousness
  • Weight loss
  • Discontinuation syndrome
    • dizziness, vertigo or muscle coordination issues
    • Skin tingling, numbness or electric shock sensations
    • Fatigue, sweating or anorexia
    • Lack of sleep, nightmares, excessive dreaming
    • Nausea, vomiting, diarrhea
    • Irritability, anxiety or agitation
    • Headaches
    • Tremors
  • Restlessness
  • Post-acute withdrawal syndrome symptoms:
    • Psychosocial dysfunction
    • Inability to experience pleasure from
    • Depression
    • Impaired interpersonal skills
    • Obsessive-compulsive behaviors
    • Feelings of guilt
    • Pessimistic thoughts
    • Inability to concentrate
    • Lack of initiative
    • Cravings
    • Memory issues
    • Emotional overreactions
    • Sensitivity to stress and pain
    • Panic
  • Increased secretion of catecholamines (chemicals responsible for flight-or-flight response, blood pressure and heart rate)

Withdrawal symptoms after stopping the daily use of clonidine are common.2 Rapid discontinuation (aka "quitting cold-turkey") can result in an immediate spike in heart rate and blood pressure. Many other symptoms mimic those experienced by patients with pheochromocytoma (a tumor on the adrenal glands).

While the most common responses involve cardiovascular changes such as irregular heartbeat and high blood pressure, more traditional withdrawal symptoms may also be experienced. Withdrawal symptoms are particularly severe for patients discontinuing from higher doses. Patients that use β-blocker following discontinuation are also at a higher risk for withdrawal symptoms.3

Fight-or-Flight

Fight-or-flight sympathetic response

Withdrawal symptoms are thought to be brought on by hyperactivity of the sympathetic nervous system. The sympathetic nervous system is responsible for flight or fight response. β-blockers bind to protein receptors similar to those bound by clonidine to prevent arrhythmias and heart attacks. β-blockers have also been shown to decrease many symptoms of clonidine withdrawal. However, they should be used with caution as they can further increase blood pressure.4

Because withdrawal can be severe, it is recommended that patients consult their physicians before discontinuing clonidine.

Clonidine Description

Clonidine (Brand names: Kapvay, Catapres, Nexiclon XR, Duraclon) is an odorless, white, bitter medication primarily used to treat high blood pressure. It is administered orally and available in tablet form at 3 different doses (0.1 mg, 0.2 mg, and 0.3 mg). However, it can also be administered intravenously. Unlike many drugs, clonidine is highly accessible when taken orally. (After the tablet is broken down following oral administration, 70-80% of the drug remains unchanged and can be absorbed into the bloodstream). It reaches peak concentrations in the body 1 to 3 hours after it is taken.5

Clonidine Medical Uses

Clonidine was approved to treat high blood pressure in 1974 by the FDA. In 2010, it was also approved to treat attention deficit disorder (ADD) in children.6 Because clonidine influences α adrenoreceptors and these receptors are concentrated in multiple regions in the brain, they are often used to treat diseases outside of blood pressure and ADD. Physicians may prescribe it for other symptoms such as: - Menstruation Pain - Tourette’s syndrome - Hot Flashes related to menopause - Smoking cessation - Withdrawal symptoms from opioid narcotics - Alcohol abuse - Restless leg syndrome - Cancer Pain - Pain following surgery in children

Clonidine Abuse

Clonidine is often used in combination with opioid narcotics such as heroin, methadone, and codeine.7 Clonidine offers several benefits to the abuser including: - Enhances the high experienced from the narcotics (fewer narcotics are needed to have the same effect) - Prolongs the high experienced from the narcotics - Easy to obtain because its abuse is not well known - Inexpensive ### Signs of clonidine addiction include Signs of clonidine addiction are similar to addiction to other drugs and alcohol.8 Some signs of addiction are: - Loss of control of clonidine use - Need for greater amounts to experience the same effects (tolerance developed) - Prioritizing clonidine uses over other responsibilities - Experiencing withdrawal following discontinuation

Although clonidine can enhance the effects of narcotics, in some instances it can be used during detox from opioids to reduce their withdrawal effects.

How Clonidine Works

Clonidine stimulates protein receptors called α adrenoreceptors in the brain stem. These receptors activate nerve cells in the sympathetic nervous system that control the heart and blood vessels. Activation of the receptors reduces signals from the brain that stimulates the heart to pump, resulting in a slower heart rate. Signals that stimulate blood vessels to constrict are also sent less frequently which allows them to relax. The combined responses lead to lower blood pressure. Some patients develop a tolerance to the blood pressure reducing effects of clonidine. Thus, readjustment of the medication may be needed over time.9

Clonidine Side Effects

Despite the potentially drastic withdrawal effects that can be experienced, clonidine is associated with very few side effects.10 These include:

  • Dry mouth
  • Drowsiness
  • Dizziness
  • Constipation
  • Sedation

These mild side effects tend to diminish over time. When used in combination with other medications, more severe side effects may be experienced such as:11

  • Fatigue
  • Fever
  • Headache
  • Pale skin color
  • Weakness
  • Withdrawal symptoms
  • Increased sensitivity to alcohol
  • Cardiovascular abnormalities
    • Slow heart rate
    • Congestive heart failure
    • Low blood pressure while standing
    • Heart palpations
  • Mental health issues
    • Delirium
    • Delusions
    • Hallucinations
    • Insomnia
    • Depression
    • Sleep disturbances
  • Abdominal pain and distress
  • Sexual dysfunction
  • Muscle cramps or pain
  • Vision problems
  • Skin irritation or rashes

Conclusion

Clonidine is an anti-hypertension medication associated with severe withdrawal symptoms. These include physical, mental and emotional withdrawal symptoms common with other drugs.

As with most other drugs, the larger the dose and the longer your course of treatment, the more severe the withdrawal symptoms will be.

A major concern with stopping clonidine is its effect on the heart and blood pressure. Although β-blockers have been shown to improve many clonidine withdrawal symptoms, they should be used with caution and under the supervision of a physician, as they can further increase blood pressure. Thus, it is imperative that patients considering discontinuing the therapy consult with a doctor prior to stopping to develop a safe and effective clonidine discontinuation plan to minimize withdrawal effects.

Reference

  1. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1429594/ 

  2. Geyskes GG, Boer P, Dorhout mees EJ. Clonidine withdrawal. Mechanism and frequency of rebound hypertension. Br J Clin Pharmacol. 1979;7(1):55-62. 

  3. Hunyor SN, Hansson L, Harrison TS, Hoobler SW. Effects of clonidine withdrawal: possible mechanisms and suggestions for management. Br Med J. 1973;2(5860):209-11. 

  4. Lilja M, Jounela AJ, Juustila HJ, Paalzow L. Abrupt and gradual change from clonidine to beta blockers in hypertension. Acta Med Scand. 1982;211(5):375-80. 

  5. Campanella C, Salvini S, Casaldi S, Chiacchiararelli F, Serra A, Di giacomo G. [Clonidine hallucinations: description of a clinical case]. Clin Ter. 2000;151(1):45-7. 

  6. Neil MJ. Clonidine: clinical pharmacology and therapeutic use in pain management. Curr Clin Pharmacol. 2011;6(4):280-7. 

  7. Beuger M, Tommasello A, Schwartz R, Clinton M. Clonidine use and abuse among methadone program applicants and patients. J Subst Abuse Treat. 1998;15(6):589-93. 

  8. Dennison SJ. Clonidine abuse among opiate addicts. Psychiatr Q. 2001;72(2):191-5. 

  9. Spiss CK, Maze M. [Adrenoreceptors]. Anaesthesist. 1985;34(1):1-10. 

  10. Kawamata T, Omote K, Yamamoto H, Toriyabe M, Wada K, Namiki A. Antihyperalgesic and side effects of intrathecal clonidine and tizanidine in a rat model of neuropathic pain. Anesthesiology. 2003;98(6):1480-3. 

  11. Max MB, Schafer SC, Culnane M, Dubner R, Gracely RH. Association of pain relief with drug side effects in postherpetic neuralgia: a single-dose study of clonidine, codeine, ibuprofen, and placebo. Clin Pharmacol Ther. 1988;43(4):363-71. 

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