α-blockers (alpha-blockers) or α-adrenergic-antagonists are pharmacological agents that act as receptor antagonists of α-adrenergic receptors (α-adrenoceptors).[1]
Contents
- 1 Classification
- 2 Uses
- 3 See also
- 4 References
Classification[edit]
- α1-blockers or antagonists act at α1-adrenoceptors
- α2-blockers or antagonists act at α2-adrenoceptors
When the term "alpha blocker" is used without further qualification, it sometimes refers to α1-blockers, and sometimes refers to agents that act at both types of receptors.[citation needed]
Examples of non-selective α-adrenergic blockers include:
- Phenoxybenzamine
- Phentolamine
- Tolazoline
- Trazodone
- Typical and atypical antipsychotics
Selective α1-adrenergic blockers include:
- Alfuzosin
- Prazosin
- Doxazosin
- Tamsulosin
- Terazosin
- Silodosin
Selective α2-adrenergic blockers include:
- Atipamezole
- Idazoxan
- Mirtazapine
- Yohimbine
The agents carvedilol and labetalol are both α- and β-blockers.
Uses[edit]
α-blockers are used in the treatment of several conditions, such as Raynaud's disease, hypertension, and scleroderma.[2]
α-blockers can also be used to treat anxiety and panic disorders, such as generalized anxiety disorder, panic disorder or posttraumatic stress disorder (PTSD). While most commonly used to treat hypertension (usually in conjunction with diuretics when other treatments are ineffective), they are also often used to treat the symptoms of BPH (benign prostatic hyperplasia). Alpha-2 adrenergic receptor agonists, such as clonidine and guanfacine, act at noradrenergic autoreceptors (presynaptic) to inhibit the firing of cells in the locus ceruleus, effectively reducing the release of brain norepinephrine.[3] Clonidine has shown promise among patients with Anxiety, Panic and Posttraumatic Stress Disorder aka PTSD in clinical trials and was used to treat severely and chronically abused and neglected preschool children. It improved disturbed behavior by reducing aggression, impulsivity, emotional outbursts, and oppositionality.[4] The following Sleep disorders of Insomnia along with theParasomnia disorders of Nightmares and /or Night Terrors aka pavor nocturnus were all reported to be reduced.
Kinzie and Leung[5] prescribed the combination of clonidine and imipramine to severely traumatized Cambodian refugees with Anxiety, Panic and PTSD. Global symptoms of PTSD were reduced among sixty-six percent and nightmares among seventy-seven percent. Guanfacine brand name Tenex produces less sedation than clonidine and thus may be better tolerated. Guanfacine reduced the trauma-related nightmares.[6] A recently completed randomized double-blind trial among veteran patients with chronic PTSD showed that augmentation with guanfacine was associated with improvement in anxiety and PTSD.
Prazosin aka Minipress is an alpha1-receptor antagonist. Raskind and colleagues[7] studied the efficacy of prazosin for PTSD among Vietnam combat veterans in a 20-week double-blind crossover protocol with a two-week drug washout to allow for return to baseline.[7] The CAPS and the Clinical Global Impressions-Change scale (CGI-C) were the primary outcome measures. Patients who were taking prazosin had a robust improvement in overall sleep quality (effect size, 1.6) and recurrent distressing dreams (effect size, 1.9). In each of the PTSD symptom clusters the effect size was medium to large: 0.7 for reexperiencing or intrusion, 0.6 for avoidance and numbing, and 0.9 for hyperarousal. The reduction in CGI-C scores (overall PTSD severity and function at endpoint) also reflected a large effect size (1.4). Prazosin appears to have promise as an effective treatment for PTSD-related sleep disturbance, including trauma-related nightmares, as well as overall Anxiety and PTSD symptoms.
See also[edit]
References[edit]
- ^ alpha-Adrenergic Blockers at the US National Library of Medicine Medical Subject Headings (MeSH)
- ^ "Alpha blockers - MayoClinic.com".
- ^ Kaplan HI, Sadock B: Synopsis of Psychiatry, 8th ed. Baltimore, Lippincott Williams & Wilkins, 1998
- ^ Harmon RJ, Riggs P: Clonidine for PTSD in preschool children. Journal of the American Academy of Child and Adolescent Psychiatry 35:1247–1249, 1996[CrossRef][Medline]
- ^ Kinzie JD, Leung P: Clonidine in Cambodian patients with posttraumatic stress disorder. Journal of Nervous and Mental Disease 177:546–550, 1989[Medline]
- ^ Horrigan JP, Barnhill LJ: The suppression of nightmares with guanfacine. Journal of Clinical Psychiatry 57:371, 1996
- ^ a b Raskind MA, Peskind ER, Kanter ED, et al: Reduction of nightmares and other PTSD symptoms in combat veterans by prazosin: a placebo controlled study. American Journal of Psychiatry 160:371–373, 2003[Abstract/Free Full Text]
Neuromodulation
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Types |
- ♦ Enzyme: Inducer
- Inhibitor
- ♦ Ion channel: Opener
- Blocker
- ♦ Receptor: Agonist
- Antagonist
- Positive allosteric modulator (PAM)
- Negative allosteric modulator (NAM)
- Inverse agonist
- ♦ Transporter [Reuptake]: Enhancer (RE)
- Inhibitor (RI)
- Releaser (RA)
- ♦ Miscellaneous: Precursor
- Cofactor
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Classes |
Enzyme
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see Enzyme inhibition
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Ion channel
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- Calcium channel blocker (CCB)
- Potassium channel blocker (PCB)
- Sodium channel blocker (SCB)
- Potassium channel opener (PCO)
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Receptor &
transporter
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BA/M
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Adrenergic
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- Adrenergic receptor agonist (α
- β (1
- 2))
- Adrenergic receptor antagonist (α (1
- 2), β)
- Adrenergic reuptake inhibitor (ARI)
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Dopaminergic
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- Dopamine receptor agonist
- Dopamine receptor antagonist
- Dopamine reuptake inhibitor (DRI)
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Histamitic
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- Histamine receptor agonist
- Histamine receptor antagonist (H1
- H2
- H3)
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Serotonergic
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- Serotonin receptor agonist
- Serotonin Receptor Antagonist (5-HT3)
- Serotonin reuptake inhibitor (SRI)
- Serotonin reuptake enhancer (SRE)
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AA
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GABAergic
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- GABA receptor agonist
- GABA receptor antagonist
- GABA reuptake inhibitor (GRI)
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Glutamitic
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- Glutamate receptor agonist (AMPA)
- Glutamate receptor antagonist (NMDA)
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Cholinergic
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- Acetylcholine receptor agonist (Muscarinic
- Nicotinic)
- Acetylcholine receptor antagonist (Muscarinic
- Nicotinic (Ganglionic
- Muscular))
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Endocannabinoid
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- Cannabinoid receptor agonist
- Cannabinoid receptor antagonist
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Opioid
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- Opioid receptor agonist
- Opioid receptor antagonist
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Other
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- Adenosine reuptake inhibitor (AdoRI)
- Angiotensin II receptor antagonist
- Endothelin receptor antagonist
- NK1 receptor antagonist
- Vasopressin receptor antagonist
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Miscellaneous
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- Cofactor (see Enzyme cofactors)
- Precursor (see Amino acids)
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Adrenergics
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Receptor ligands
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α1
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- Agonists: 5-FNE
- 6-FNE
- Amidephrine
- Anisodamine
- Anisodine
- Cirazoline
- Dipivefrine
- Dopamine
- Ephedrine
- Epinephrine
- Etilefrine
- Ethylnorepinephrine
- Indanidine
- Levonordefrin
- Metaraminol
- Methoxamine
- Methyldopa
- Midodrine
- Naphazoline
- Norepinephrine
- Octopamine
- Oxymetazoline
- Phenylephrine
- Phenylpropanolamine
- Pseudoephedrine
- Synephrine
- Tetrahydrozoline
Antagonists: Abanoquil
- Adimolol
- Ajmalicine
- Alfuzosin
- Amosulalol
- Arotinolol
- Atiprosin
- Benoxathian
- Buflomedil
- Bunazosin
- Carvedilol
- CI-926
- Corynanthine
- Dapiprazole
- DL-017
- Domesticine
- Doxazosin
- Eugenodilol
- Fenspiride
- GYKI-12,743
- GYKI-16,084
- Hydroxyzine
- Indoramin
- Ketanserin
- L-765,314
- Labetalol
- Mephendioxan
- Metazosin
- Monatepil
- Moxisylyte
- Naftopidil
- Nantenine
- Neldazosin
- Nicergoline
- Niguldipine
- Pelanserin
- Phendioxan
- Phenoxybenzamine
- Phentolamine
- Piperoxan
- Prazosin
- Quinazosin
- Ritanserin
- RS-97,078
- SGB-1,534
- Silodosin
- SL-89.0591
- Spiperone
- Talipexole
- Tamsulosin
- Terazosin
- Tibalosin
- Tiodazosin
- Tipentosin
- Tolazoline
- Trimazosin
- Upidosin
- Urapidil
- Zolertine
- Note that many TCAs, TeCAs, antipsychotics, ergolines, and some piperazines like buspirone and trazodone all antagonize α1-adrenergic receptors as well, which contributes to their side effects such as orthostatic hypotension.
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α2
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- Agonists: (R)-3-Nitrobiphenyline
- 4-NEMD
- 6-FNE
- Amitraz
- Apraclonidine
- Brimonidine
- Cannabivarin
- Clonidine
- Detomidine
- Dexmedetomidine
- Dihydroergotamine
- Dipivefrine
- Dopamine
- Ephedrine
- Ergotamine
- Epinephrine
- Esproquin
- Etilefrine
- Ethylnorepinephrine
- Guanabenz
- Guanfacine
- Guanoxabenz
- Levonordefrin
- Lofexidine
- Medetomidine
- Methyldopa
- Mivazerol
- Naphazoline
- Norepinephrine
- Oxymetazoline
- Phenylpropanolamine
- Piperoxan
- Pseudoephedrine
- Rilmenidine
- Romifidine
- Talipexole
- Tetrahydrozoline
- Tizanidine
- Tolonidine
- Urapidil
- Xylazine
- Xylometazoline
Antagonists: 1-PP
- Adimolol
- Aptazapine
- Atipamezole
- BRL-44408
- Buflomedil
- Cirazoline
- Efaroxan
- Esmirtazapine
- Fenmetozole
- Fluparoxan
- GYKI-12,743
- GYKI-16,084
- Idazoxan
- Mianserin
- Mirtazapine
- MK-912
- NAN-190
- Olanzapine
- Phentolamine
- Phenoxybenzamine
- Piperoxan
- Piribedil
- Rauwolscine
- Rotigotine
- SB-269,970
- Setiptiline
- Spiroxatrine
- Sunepitron
- Tolazoline
- Yohimbine
* Note that many atypical antipsychotics and azapirones like buspirone (via metabolite 1-PP) antagonize α2-adrenergic receptors as well.
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β
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Reuptake inhibitors
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NET
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- Selective norepinephrine reuptake inhibitors: Amedalin
- Atomoxetine (Tomoxetine)
- Ciclazindol
- Daledalin
- Edivoxetine
- Esreboxetine
- Lortalamine
- Mazindol
- Nisoxetine
- Reboxetine
- Talopram
- Talsupram
- Tandamine
- Viloxazine; Norepinephrine-dopamine reuptake inhibitors: Amineptine
- Bupropion (Amfebutamone)
- Fencamine
- Fencamfamine
- Lefetamine
- Levophacetoperane
- LR-5182
- Manifaxine
- Methylphenidate
- Nomifensine
- O-2172
- Radafaxine; Serotonin-norepinephrine reuptake inhibitors: Bicifadine
- Desvenlafaxine
- Duloxetine
- Eclanamine
- Levomilnacipran
- Milnacipran
- Sibutramine
- Venlafaxine; Serotonin-norepinephrine-dopamine reuptake inhibitors: Brasofensine
- Diclofensine
- DOV-102,677
- DOV-21,947
- DOV-216,303
- JNJ-7925476
- JZ-IV-10
- Methylnaphthidate
- Naphyrone
- NS-2359
- PRC200-SS
- SEP-225,289
- SEP-227,162
- Tesofensine; Tricyclic antidepressants: Amitriptyline
- Butriptyline
- Cianopramine
- Clomipramine
- Desipramine
- Dosulepin
- Doxepin
- Imipramine
- Lofepramine
- melitracen
- Nortriptyline
- Protriptyline
- Trimipramine; Tetracyclic antidepressants: Amoxapine
- Maprotiline
- Mianserin
- Oxaprotiline
- Setiptiline; Others: Cocaine
- CP-39,332
- Ethanol
- EXP-561
- Fezolamine
- Ginkgo biloba
- Indeloxazine
- Nefazodone
- Nefopam
- Pridefrine
- Tapentadol
- Tedatioxetine
- Teniloxazine
- Tofenacin
- Tramadol
- Ziprasidone
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VMAT
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- Ibogaine
- Reserpine
- Tetrabenazine
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Enzyme inhibitors
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Anabolism
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PAH
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TH
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- 3-Iodotyrosine
- Aquayamycin
- Bulbocapnine
- Metirosine
- Oudenone
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AAAD
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- Benserazide
- Carbidopa
- DFMD
- Genistein
- Methyldopa
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DBH
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- Bupicomide
- Disulfiram
- Dopastin
- Fusaric acid
- Nepicastat
- Phenopicolinic acid
- Tropolone
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PNMT
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- CGS-19281A
- SKF-64139
- SKF-7698
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Catabolism
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MAO
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- Nonselective: Benmoxin
- Caroxazone
- Echinopsidine
- Furazolidone
- Hydralazine
- Indantadol
- Iproclozide
- Iproniazid
- Isocarboxazid
- Isoniazid
- Linezolid
- Mebanazine
- Metfendrazine
- Nialamide
- Octamoxin
- Paraxazone
- Phenelzine
- Pheniprazine
- Phenoxypropazine
- Pivalylbenzhydrazine
- Procarbazine
- Safrazine
- Tranylcypromine; MAO-A selective: Amiflamine
- Bazinaprine
- Befloxatone
- Brofaromine
- Cimoxatone
- Clorgiline
- Eprobemide
- Esuprone
- Harmala alkaloids (Harmine,
- Harmaline
- Tetrahydroharmine
- Harman
- Norharman, etc)
- Methylene blue
- Metralindole
- Minaprine
- Moclobemide
- Pirlindole
- Sercloremine
- Tetrindole
- Toloxatone
- Tyrima; MAO-B selective:
- Ladostigil
- Lazabemide
- Milacemide
- Mofegiline
- Pargyline
- Rasagiline
- Safinamide
- Selegiline (also D-Deprenyl)
* Note that MAO-B inhibitors also influence norepinephrine/epinephrine levels since they inhibit the breakdown of their precursor dopamine.
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COMT
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- Entacapone
- Nitecapone
- Tolcapone
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Others
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Precursors
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- L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa) → Dopamine
- L-DOPS (Droxidopa)
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Cofactors
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- Ferrous Iron (Fe2+)
- S-Adenosyl-L-Methionine
- Vitamin B3 (Niacin
- Nicotinamide → NADPH)
- Vitamin B6 (Pyridoxine
- Pyridoxamine
- Pyridoxal → Pyridoxal Phosphate)
- Vitamin B9 (Folic acid → Tetrahydrofolic acid)
- Vitamin C (Ascorbic acid)
- Zinc (Zn2+)
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Others
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- Activity enhancers: BPAP
- PPAP; Release blockers: Bethanidine
- Bretylium
- Guanadrel
- Guanazodine
- Guanclofine
- Guanethidine
- Guanoxan; Toxins: 6-OHDA
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List of adrenergic drugs
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Drugs used in benign prostatic hypertrophy (G04C)
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5α-reductase inhibitors |
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Alpha blockers (α1) |
- Alfuzosin
- Doxazosin
- Silodosin
- Tamsulosin
- Terazosin
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Herbals |
- Pygeum africanum
- Saw palmetto extract
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Other |
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noco/cong/tumr, sysi/epon
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