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__NOTOC__
__NOTOC__
{{Methyldopa}}
{{Clonidine}}
{{CMG}}; {{AE}}
{{CMG}}; {{AE}} {{PB}}


'''''For patient information about Methyldopa, click [[Methyldopa (patient information)|here]].'''''
'''''For patient information about Clonidine, click [[Clonidine (patient information)|here]]'''''


{{SB}}
{{SB}}
Methylodopa<sup>®</sup>


==Overview==
==Overview==
'''Methyldopa''' or '''alpha-methyldopa''' (brand names '''Aldomet®''', '''Apo-Methyldopa®''', '''Dopamet®''', '''Novomedopa®''') is a centrally-acting adrenergic [[antihypertensive]] medication. Its use is now deprecated following introduction of alternative safer classes of agents. However it continues to have a role in otherwise difficult to treat hypertension and [[pregnancy-induced hypertension]].
 
Not to be confused with [[clomifene]], [[clonazepam]] ([[Klonopin]]), or [[clozapine]].
 
Clonidine (trade names Catapres, Kapvay, Nexiclon and others) is a sympatholytic medication used to treat high blood pressure, [[ADHD]], [[anxiety]]/[[panic disorder]], and certain pain conditions. It is classified as a centrally acting α2 adrenergic agonist. An alternative hypothesis that has been proposed is that clonidine acts centrally as an [[imidazoline]] receptor agonist.
 
==Category==
==Category==
Central adrengeric antihypertensives.


==FDA Package Insert==
Anti Migraine Preparation.
 
====CATAPRES====


====Methyldopa tablet<sup>®</sup>====
'''  [[CATAPRES indications and usage|Indications and Usage]]'''
'''| [[CATAPRES dosage and administration|Dosage and Administration]]'''
'''| [[CATAPRES dosage forms and strengths|Dosage Forms and Strengths]]'''
'''| [[CATAPRES contraindications|Contraindications]]'''
'''| [[CATAPRES warnings and precautions|Warnings and Precautions]]'''
'''| [[CATAPRES adverse reactions|Adverse Reactions]]'''
'''| [[CATAPRES drug interactions|Drug Interactions]]'''
'''| [[CATAPRES use in specific populations|Use in Specific Populations]]'''
'''| [[CATAPRES overdosage|Overdosage]]'''
'''| [[CATAPRES description|Description]]'''
'''| [[CATAPRES clinical pharmacology|Clinical Pharmacology]]'''
'''| [[CATAPRES nonclinical toxicology|Nonclinical Toxicology]]'''
'''| [[CATAPRES clinical studies|Clinical Studies]]'''
'''| [[CATAPRES how supplied storage and handling|How Supplied/Storage and Handling]]'''
'''| [[CATAPRES patient counseling information|Patient Counseling Information]]'''
'''| [[CATAPRES labels and packages|Labels and Packages]]'''


====CLONIDINE patch====


''' [[Methyldopa tablet indications and usage|Indications and Usage]]'''
'''| [[CLONIDINE patch indications and usage|Indications and Usage]]'''
'''| [[Methyldopa tablet dosage and administration|Dosage and Administration]]'''
'''| [[CLONIDINE patch dosage and administration|Dosage and Administration]]'''
'''| [[Methyldopa tablet dosage forms and strengths|Dosage Forms and Strengths]]'''
'''| [[CLONIDINE patch dosage forms and strengths|Dosage Forms and Strengths]]'''
'''| [[Methyldopa tablet contraindications|Contraindications]]'''
'''| [[CLONIDINE patch contraindications|Contraindications]]'''
'''| [[Methyldopa tablet warnings |Warnings ]]'''
'''| [[CLONIDINE patch warnings and precautions|Warnings and Precautions]]'''
'''| [[Methyldopa tablet precautions| Precautions]]'''
'''| [[CLONIDINE patch adverse reactions|Adverse Reactions]]'''
'''| [[Methyldopa tablet adverse reactions|Adverse Reactions]]'''
'''| [[CLONIDINE patch drug interactions|Drug Interactions]]'''
'''| [[Methyldopa tablet drug interactions|Drug Interactions]]'''
'''| [[CLONIDINE patch use in specific populations|Use in Specific Populations]]'''
'''| [[Methyldopa tablet use in specific populations|Use in Specific Populations]]'''
'''| [[CLONIDINE patch overdosage|Overdosage]]'''
'''| [[Methyldopa tablet overdosage|Overdosage]]'''
'''| [[CLONIDINE patch description|Description]]'''
'''| [[Methyldopa tablet description|Description]]'''
'''| [[CLONIDINE patch clinical pharmacology|Clinical Pharmacology]]'''
'''| [[Methyldopa tablet clinical pharmacology|Clinical Pharmacology]]'''
'''| [[CLONIDINE patch nonclinical toxicology|Nonclinical Toxicology]]'''
'''| [[Methyldopa tablet nonclinical toxicology|Nonclinical Toxicology]]'''
'''| [[CLONIDINE patch clinical studies|Clinical Studies]]'''
'''| [[Methyldopa tablet clinical studies|Clinical Studies]]'''
'''| [[CLONIDINE patch how supplied storage and handling|How Supplied/Storage and Handling]]'''
'''| [[Methyldopa tablet how supplied storage and handling|How Supplied/Storage and Handling]]'''
'''| [[CLONIDINE patch patient counseling information|Patient Counseling Information]]'''
'''| [[Methyldopa tablet patient counseling information|Patient Counseling Information]]'''
'''| [[CLONIDINE patch labels and packages|Labels and Packages]]'''
'''| [[Methyldopa tablet labels and packages|Labels and Packages]]'''


====Methyldopa injection<sup>®</sup>====
====DURACLON====
''' [[Methyldopa injection indications and usage|Indications and Usage]]'''
 
'''| [[Methyldopa injection dosage and administration|Dosage and Administration]]'''
'''| [[DURACLON indications and usage|Indications and Usage]]'''
'''| [[Methyldopa injection dosage forms and strengths|Dosage Forms and Strengths]]'''
'''| [[DURACLON dosage and administration|Dosage and Administration]]'''
'''| [[Methyldopa injection contraindications|Contraindications]]'''
'''| [[DURACLON dosage forms and strengths|Dosage Forms and Strengths]]'''
'''| [[Methyldopa injection warnings| Warnings]]'''
'''| [[DURACLON contraindications|Contraindications]]'''
'''| [[Methyldopa injection precautions|Precautions]]'''
'''| [[DURACLON warnings and precautions|Warnings and Precautions]]'''
'''| [[Methyldopa injection adverse reactions|Adverse Reactions]]'''
'''| [[DURACLON adverse reactions|Adverse Reactions]]'''
'''| [[Methyldopa injection drug interactions|Drug Interactions]]'''
'''| [[DURACLON drug interactions|Drug Interactions]]'''
'''| [[Methyldopa injection use in specific populations|Use in Specific Populations]]'''
'''| [[DURACLON use in specific populations|Use in Specific Populations]]'''
'''| [[Methyldopa injection overdosage|Overdosage]]'''
'''| [[DURACLON overdosage|Overdosage]]'''
'''| [[Methyldopa injection description|Description]]'''
'''| [[DURACLON description|Description]]'''
'''| [[Methyldopa injection clinical pharmacology|Clinical Pharmacology]]'''
'''| [[DURACLON clinical pharmacology|Clinical Pharmacology]]'''
'''| [[Methyldopa injection nonclinical toxicology|Nonclinical Toxicology]]'''
'''| [[DURACLON nonclinical toxicology|Nonclinical Toxicology]]'''
'''| [[Methyldopa injection clinical studies|Clinical Studies]]'''
'''| [[DURACLON clinical studies|Clinical Studies]]'''
'''| [[Methyldopa injection how supplied storage and handling|How Supplied/Storage and Handling]]'''
'''| [[DURACLON how supplied storage and handling|How Supplied/Storage and Handling]]'''
'''| [[Methyldopa injection patient counseling information|Patient Counseling Information]]'''
'''| [[DURACLON patient counseling information|Patient Counseling Information]]'''
'''| [[Methyldopa injection labels and packages|Labels and Packages]]'''
'''| [[DURACLON labels and packages|Labels and Packages]]'''


==Mechanism of action==
==Mechanism of action==
Methyldopa has variable absorption from the gut of approximately 50%. It is metabolized in the [[intestine]]s and [[liver]]; its metabolite alpha-methylnorepineprine acts in the [[brain]] to stimulate [[alpha-adrenergic receptor]]s decreasing [[total peripheral resistance]]. It is [[excretion|excreted]] in [[urine]].
Clonidine treats high blood pressure by stimulating [[Alpha-2 adrenergic receptor|α<sub>2</sub>-receptors]] in the brain, which decreases [[peripheral vascular resistance]], lowering blood pressure. It has specificity towards the [[presynaptic]] α<sub>2</sub>-receptors in the vasomotor center in the [[brainstem]]. This binding decreases presynaptic [[calcium]] levels, thus inhibiting the release of [[norepinephrine]] (NE). The net effect is a decrease in sympathetic tone.
 
It has also been proposed that the antihypertensive effect of clonidine is due to agonism on the I<sub>1</sub>-receptor ([[imidazoline receptor]]), which mediates the sympatho-inhibitory actions of imidazolines to lower blood pressure.


Methyldopa, in its active metabolite form, leads to increased alpha-2 receptor-mediated inhibition of SNS (centrally and peripherally), allowing PSNS tone to increase. Such activity leads to a decrease in total peripheral resistance (TPR) and [[cardiac output]].
Its mechanism of action in the treatment of [[ADHD]] is to increase noradrenergic tone in the [[prefrontal cortex]] (PFC) directly by binding to postsynaptic [[alpha-2A adrenergic receptor|α<sub>2A</sub> adrenergic receptors]] and indirectly by increasing [[norepinephrine]] input from the [[locus coeruleus]].<ref name="dailymed.nlm.nih.gov">{{Cite web  | last =  | first =  | title = CATAPRES (CLONIDINE HYDROCHLORIDE) TABLET [BOEHRINGER INGELHEIM PHARMACEUTICALS INC.] | url = http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=d7f569dc-6bed-42dc-9bec-940a9e6b090d | publisher =  | date =  | accessdate = 5 February 2014 }}</ref>


If methyldopa is abruptly withdrawn, rebound hypertension happens. This results because the long term use of methyldopa lowers the sensitivity of presynaptic alpha 2 receptors: the release of [[norepinephrine]] (NE) from sympathetic nerve endings is modulated by NE itself acting on the  presynaptic alpha 2 autoreceptors thus inhibiting its own release. The discontinuation of methyldopa removes the inhibition on NE release leading to excessive NE release from the SNS and the rebound hypertension.<ref name="dailymed.nlm.nih.gov">{{Cite web  | last =  | first =  | title = METHYLDOPA TABLET [CARDINAL HEALTH] | url = http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=d87d63fd-48f7-4130-af03-5e263c338fe4 | publisher =  | date =  | accessdate = 10 March 2014 }}</ref>
{| class="wikitable"
! Receptor !! K<sub>i</sub> (nM)
|-
| [[Alpha-1A adrenergic receptor|α<sub>1A</sub>]] || 316.2278
|-
| [[Alpha-1B adrenergic receptor|α<sub>1B</sub>]] || 316.2278
|-
| [[Alpha-1D adrenergic receptor|α<sub>1D</sub>]] || 125.8925
|-
| [[Alpha-2A adrenergic receptor|α<sub>2A</sub>]] || 42.92
|-
| [[Alpha-2B adrenergic receptor|α<sub>2B</sub>]] || 106.31
|-
| [[Alpha-2C adrenergic receptor|α<sub>2C</sub>]] || 233.1
|}


==References==
==References==

Revision as of 14:09, 16 July 2014

Clonidine
CATAPRES® FDA Package Insert
Indications and Usage
Dosage and Administration
Dosage Forms and Strengths
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Overdosage
Description
Clinical Pharmacology
Nonclinical Toxicology
Clinical Studies
How Supplied/Storage and Handling
Patient Counseling Information
Labels and Packages
CLONIDINE patch ® FDA Package Insert
Indications and Usage
Dosage and Administration
Dosage Forms and Strengths
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Overdosage
Description
Clinical Pharmacology
Nonclinical Toxicology
Clinical Studies
How Supplied/Storage and Handling
Patient Counseling Information
Labels and Packages
DURACLON (clonidine hydrochloride) injection® FDA Package Insert
Indications and Usage
Dosage and Administration
Dosage Forms and Strengths
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Overdosage
Description
Clinical Pharmacology
Nonclinical Toxicology
Clinical Studies
How Supplied/Storage and Handling
Patient Counseling Information
Labels and Packages
Clinical Trials on Clonidine
ClinicalTrials.gov

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Pratik Bahekar, MBBS [2]

For patient information about Clonidine, click here

Synonyms / Brand Names:

Overview

Not to be confused with clomifene, clonazepam (Klonopin), or clozapine.

Clonidine (trade names Catapres, Kapvay, Nexiclon and others) is a sympatholytic medication used to treat high blood pressure, ADHD, anxiety/panic disorder, and certain pain conditions. It is classified as a centrally acting α2 adrenergic agonist. An alternative hypothesis that has been proposed is that clonidine acts centrally as an imidazoline receptor agonist.

Category

Anti Migraine Preparation.

CATAPRES

Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages

CLONIDINE patch

| Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages

DURACLON

| Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages

Mechanism of action

Clonidine treats high blood pressure by stimulating α2-receptors in the brain, which decreases peripheral vascular resistance, lowering blood pressure. It has specificity towards the presynaptic α2-receptors in the vasomotor center in the brainstem. This binding decreases presynaptic calcium levels, thus inhibiting the release of norepinephrine (NE). The net effect is a decrease in sympathetic tone.

It has also been proposed that the antihypertensive effect of clonidine is due to agonism on the I1-receptor (imidazoline receptor), which mediates the sympatho-inhibitory actions of imidazolines to lower blood pressure.

Its mechanism of action in the treatment of ADHD is to increase noradrenergic tone in the prefrontal cortex (PFC) directly by binding to postsynaptic α2A adrenergic receptors and indirectly by increasing norepinephrine input from the locus coeruleus.[1]

Receptor Ki (nM)
α1A 316.2278
α1B 316.2278
α1D 125.8925
α2A 42.92
α2B 106.31
α2C 233.1

References

  1. ↑ "CATAPRES (CLONIDINE HYDROCHLORIDE) TABLET [BOEHRINGER INGELHEIM PHARMACEUTICALS INC.]". Retrieved 5 February 2014.
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