Products
Sympathomimetics are commercially available, for example, in the form of tablets, capsules, granules, injectable solutions, eye drops, and nasal sprays.
Structure and properties
Sympathomimetics are structurally derived from the natural neurotransmitters epinephrine and norepinephrine.
Effects
Sympathomimetics have sympathomimetic properties, meaning that they promote the effects of the sympathetic nervous system, a portion of the autonomic (autonomic) nervous system. Their effects are based either on direct agonism at α- or β-adrenoceptors (GPCR) or on increasing the concentration of epinephrine or norepinephrine, for example, by interaction with synaptic vesicles, by inhibition of metabolism, or by reuptake inhibition. Thus, a distinction can be made between direct and indirect sympathomimetics. Sympathomimetics differ in their selectivity for the α- or β-adrenoceptors and their subtypes. Their pharmacological effects include (“Fight or Flight”):
- Pupillary dilation
- Increased heart rate, contractility and conduction velocity at the heart.
- Vascular constriction
- Decrease in motility and tone in the digestive tract.
- Bronchodilatation
- Renin secretion
- Central stimulation
Dosage
According to the professional information. Sympathomimetics are administered both systemically and topically.
Abuse
Sympathomimetics can be abused as stimulants, doping agents, anabolic steroids, intoxicants, and smart drugs.
Agents
Selection of sympathomimetic agents: Inhalants, beta2-sympathomimetics:
- Fenoterol (Berodual N)
- Formoterol (Foradil, Oxis)
- Indacaterol (Onbrez Breezhaler)
- Olodaterol (Striverdi Respimat)
- Salbutamol (Ventolin)
- Salmeterol (Serevent)
- Terbutaline (Bricanyl)
- Vilanterol (eg, Relvar Ellipta with fluticasone furoate).
Injections and infusions:
- Adrenaline (various providers)
- Dobutamine (Dobutrex)
- Dopamine (Dopamine Sintetica)
- Hexoprenaline (Gynipral, solution for injection).
- Isoprenaline (out of trade)
- Norepinephrine (various suppliers)
Amphetamines and other stimulants:
- Amphetamine
- Cocaine
- Dexamphetamine (dexamine, out of commerce in many countries).
- Dexmethylphenidate (Focalin)
- Cath, cathinone
- Lisdexamphetamine (Elvanse)
- Methamphetamine (“Crystal Meth”)
- Methylphenidate (e.g., Ritalin, Concerta, generics).
- Phentermine (Adipex, out of trade).
Low blood pressure:
- Etilefrin (Effortil)
- Midodrine (Gutron)
- Norfenefrin (Ortho-Maren, out of commerce).
- Oxedrine (Sympalept, out of trade)
Decongestant nasal sprays:
- Oxymetazoline (Nasivin)
- Phenylephrine (Vibrocil)
- Tuaminoheptane (Rinofluimucil)
- Xylometazoline (e.g., Otrivin, Triofan, generics).
Cold remedies:
- Ephedrine
- Methylephedrine (Tossamine plus)
- Phenylephrine (NeoCitran)
- Pseudoephedrine (Pretuval)
Eye drops:
- Naphazoline
- Phenylephrine
- Tetryzoline (Collypan, Visine)
Irritable bladder:
- Mirabegron (Betmiga)
Other:
- Phenylpropanolamine
Other agents such as the various antidepressants have sympathomimetic properties.
Indications
Major indications for sympathomimetics (selection):
- Attention deficit hyperactivity disorder (ADHD).
- Allergy, hay fever, anaphylaxis
- Asthma, COPD, bronchitis
- Conjunctivitis
- Hypotension (Low blood pressure)
- Cardiopulmonary resuscitation
- Fatigue
- Narcolepsy
- Cold, rhinitis, sinusitis
- As a contraceptive
- Overweight (no longer on the market)
Contraindications
Contraindications include (selection):
- Hypersensitivity
- High blood pressure (hypertension)
- Hyperthyroidism
- Pheochromocytoma
- Narrow-angle glaucoma
- Prostate enlargement
- Coronary artery disease, heart disease
Full precautions can be found in the drug label.
Interactions
Drug-drug interactions occur with other sympathomimetic agents and with agents that inhibit their breakdown (eg, MAO inhibitors). Sympatholytics may reverse the effects of sympathomimetics.
Adverse effects
Possible adverse effects include:
- Sleep disturbance
- Central disorders such as headaches, dizziness, irritability, nervousness, anxiety.
- Rapid heart rate, cardiac arrhythmias, palpitations, angina pectoris.
- High blood pressure
- Gastrointestinal disorders such as nausea and abdominal pain.
- Vascular constriction, goose bumps, feeling cold, pallor.
- Urinary retention
- Hyperglycemia
