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Search results for "Pharmacologic Substance[C1909]|Agent Affecting Nervous System[C78272]" in comments (approximate match)
Status:
US Approved OTC
Source:
21 CFR 336.10(a) antiemetic cyclizine hydrochloride
Source URL:
First approved in 1953
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Cyclizine (cyclizine hydrochloride, Valoid®) is a histamine H1 antagonist of the piperazine class which is characterised by a low incidence of drowsiness. It possesses anticholinergic and antiemetic properties. The exact mechanism by which cyclizin (cyclizine hydrochloride, Valoid®) can prevent or suppress both nausea and vomiting from various causes is unknown. It increases lower oesophageal sphincter tone and reduces the sensitivity of the labyrinthine apparatus. It may inhibit the part of the midbrain known collectively as the emetic centre.
Status:
US Approved OTC
Source:
21 CFR 341.20(b)(9) cough/cold:nasal decongestant propylhexedrine
Source URL:
First approved in 1949
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Propylhexedrine is considered to be an agonist of alpha-adrenergic receptors. It is effective as a topical vasoconstrictor. The primary medicinal use of Benzedrex (Propylhexedrine inhaler) propylhexedrine is temporary symptomatic relief of nasal decongestion due to colds, allergies and allergic rhinitis. Structurally and pharmacologically related to amphetamine.Exact mechanism of action unknown but thought to be similar to amphetamine. When used as a nasal inhaler for this indication, propylhexedrine reduces nasal airway resistance without producing rebound congestion. Abuse does not occur by nasal inhalation; however, a small amount of abuse of the propylhexedrine containing nasal inhalers occurs by oral ingestion of the contents of the inhaler or by intravenous injection. Propylhexedrine is a central nervous system (CNS) stimulant of low abuse potential, a stimulant of low preference for stimulant abusers compared with amphetamine, methylphenidate, phenmetrazine.
Status:
US Approved OTC
Source:
21 CFR 336.10(b) antiemetic dimenhydrinate
Source URL:
First approved in 1949
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
US Approved OTC
Source:
21 CFR 348.10(a)(2) external analgesic:male genital desensitizer lidocaine
Source URL:
First approved in 1948
Source:
NDA006488
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Lidocaine is a local anesthetic and cardiac depressant used to numb tissue in a specific area and for management of cardiac arrhythmias, particularly those of ventricular origins, such as occur with acute myocardial infarction. Lidocaine alters signal conduction in neurons by blocking the fast voltage-gated Na+ channels in the neuronal cell membrane responsible for signal propagation. With sufficient blockage, the membrane of the postsynaptic neuron will not depolarize and will thus fail to transmit an action potential. This creates the anesthetic effect by not merely preventing pain signals from propagating to the brain, but by stopping them before they begin. Careful titration allows for a high degree of selectivity in the blockage of sensory neurons, whereas higher concentrations also affect other modalities of neuron signaling. Lidocaine exerts an antiarrhythmic effect by increasing the electrical stimulation threshold of the ventricle during diastole. In usual therapeutic doses, lidocaine hydrochloride produces no change in myocardial contractility, in systemic arterial pressure, or an absolute refractory period. The efficacy profile of lidocaine as a local anesthetic is characterized by a rapid onset of action and intermediate duration of efficacy. Therefore, lidocaine is suitable for infiltration, block, and surface anesthesia. Longer-acting substances such as bupivacaine are sometimes given preference for spinal and epidural anesthesias; lidocaine, though, has the advantage of a rapid onset of action. Lidocaine is also the most important class-1b antiarrhythmic drug; it is used intravenously for the treatment of ventricular arrhythmias (for acute myocardial infarction, digoxin poisoning, cardioversion, or cardiac catheterization) if amiodarone is not available or contraindicated. Lidocaine should be given for this indication after defibrillation, CPR, and vasopressors have been initiated. A routine preventative dose is no longer recommended after a myocardial infarction as the overall benefit is not convincing. Inhaled lidocaine can be used as a cough suppressor acting peripherally to reduce the cough reflex. This application can be implemented as a safety and comfort measure for patients who have to be intubated, as it reduces the incidence of coughing and any tracheal damage it might cause when emerging from anesthesia. Adverse drug reactions (ADRs) are rare when lidocaine is used as a local anesthetic and is administered correctly. Most ADRs associated with lidocaine for anesthesia relate to administration technique (resulting in systemic exposure) or pharmacological effects of anesthesia, and allergic reactions only rarely occur. Systemic exposure to excessive quantities of lidocaine mainly result in a central nervous system (CNS) and cardiovascular effects – CNS effects usually occur at lower blood plasma concentrations and additional cardiovascular effects present at higher concentrations, though cardiovascular collapse may also occur with low concentrations.
Status:
US Approved OTC
Source:
21 CFR 341.14(a)(5) cough/cold:antitussive diphenhydramine citrate
Source URL:
First approved in 1946
Source:
BENADRYL by MCNEIL CONS
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Diphenhydramine is an antihistamine which is used in the combination with naproxen sodium for the relief of occasional sleeplessness when associated with minor aches and pains. Diphenhydramine has a role nighttime sleep-aid and naproxen sodium is a pain reliever. In addition, diphenhydramine used in relieving symptoms in patients with moderate-to-severe seasonal allergic rhinitis. Diphenhydramine acts as an antagonist of histamine H1 receptor. Besides, was shown potential to repurpose diphenhydramine as an anti-melanoma therapeutic agent, it induces melanoma cell apoptosis by suppressing STAT3/MCL-1 survival signaling pathway.
Status:
US Approved OTC
Source:
21 CFR 341.20(b)(6) cough/cold:nasal decongestant naphazoline hydrochloride
Source URL:
First approved in 1942
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Naphazoline is a direct acting sympathomimetic adrenergic alpha-agonist used to induce systemic vasoconstriction, thereby decreasing nasal congestion and inducing constriction around the conjunctiva. The sympathomimetic action of Naphazoline constricts the smaller arterioles of the nasal passages, producing a decongesting effect. Naphazoline ophthalmic causes constriction of blood vessels in the eyes. It also decreases itching and irritation of the eyes. aphazoline constricts the vascular system of the conjunctiva. It is presumed that this effect is due to direct stimulation action of the drug upon the alpha adrenergic receptors in the arterioles of the conjunctiva resulting in decreased conjunctival congestion. Naphazoline belongs to the imidazoline class of sympathomimetics. Naphazoline is a direct acting sympathomimetic drug, which acts on alpha-adrenergic receptors in the arterioles of the nasal mucosa. This activates the adrenal system to yield systemic vasoconstrction. In producing vasoconstriction, the result is a decrease in blood flow in the nasal passages and consequently decreased nasal congestion. The vasoconstriction means that there is less pressure in the capillaries and less water can filter out, thus less discharge is made. Naphazoline is primarily indicated in conditions like Corneal vascularity, Hyperaemia, Itching, Nasal congestion, and can also be given in adjunctive therapy as an alternative drug of choice in Sinusitis.
Status:
US Approved OTC
Source:
21 CFR 346.12(d) anorectal:vasoconstrictor phenylephrine hydrochloride
Source URL:
First marketed in 1934
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Berefrine (also known as phenylephrine oxazolidine), a prodrug of phenylephrine, is a mydriatic agent. Berefrine was developed for improving ocular absorption and reducing systemic side effects.
Status:
US Approved OTC
Source:
21 CFR 346.10(i) anorectal:local anesthetic tetracaine hydrochloride
Source URL:
First marketed in 1932
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Tetracaine (INN, also known as amethocaine; trade name Pontocaine. Ametop and Dicaine) is a potent local anesthetic of the ester group. It is mainly used topically in ophthalmology and as an antipruritic, and it has been used in spinal anesthesia. Tetracaine blocks sodium ion channels required for the initiation and conduction of neuronal impulses thereby affecting local anesthesia. In biomedical research, tetracaine is used to alter the function of calcium release channels (ryanodine receptors) that control the release of calcium from intracellular stores. Tetracaine is an allosteric blocker of channel function. At low concentrations, tetracaine causes an initial inhibition of spontaneous calcium release events, while at high concentrations, tetracaine blocks release completely.
Status:
US Approved OTC
Source:
21 CFR 346.10(c) anorectal:local anesthetic dibucaine
Source URL:
First marketed in 1930
Source:
Dibucaine; Nupercaine by Society of Chemical Industry in Basle, Basle, Switzerland (Ciba Company, Inc., New York, distributor).
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Dibucaine is used as a local anesthetic for surface anesthesia. It is one of the most potent and toxic of the long-acting local anesthetics and its parenteral use is restricted to spinal anesthesia. Dibucaine is used to temporarily relieve pain and itching due to: hemorrhoids or other anorectal disorders, sunburn, minor burns, minor cuts; scrapes, insect bites, minor skin irritation. This drug acts via blocking of nerve impulses by decreasing the neuronal membrane's permeability to sodium ions through sodium channel blocking. This reversibly stabilizes the membrane and inhibits depolarization, resulting in the failure of a propagated action potential and subsequent conduction blockade.
Status:
US Approved OTC
Source:
21 CFR 346.12(a) anorectal:vasoconstrictor ephedrine sulfate
Source URL:
First marketed in 1928
Source:
Ephetonine by Merck
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Ephedrine (l-form) is an alkaloid, which was initially purified from Ephedra plant. The extract form Ephedra has been used in China for medicinal purposes for several thousand years. Ephedrine acts as an agonist at alpha- and beta-adrenergic receptors and indirectly causes the release of norepinephrine from sympathetic neurons. The drug crosses the blood brain barrier and stimulates the central nervous system. Ephedrine products are now banned in many countries, as they are a major source for the production of the addictive compound methamphetamine. FDA has approved ephedrine only for the treatment of clinically important hypotension occurring in the setting of anesthesia.