Antihistamines antiemetic action

Mechanism of Action A phenothiazine that acts as an antihistamine, antiemetic, and CNS-antipsychotiC typical hypnotic. As an antihistamine, inhibits histamine at histamine receptor sites. As an antiemetic, diminishes vestibular stimulation, depresses labyrinthine function, and acts on the chemoreceptor trigger zone. As a sedative-hypnotic, produces CNS depression by decreasing stimulation to the brainstem reticular formation. Therapeutic Effect Prevents allergic responses mediated by histamine, such as rhinitis, urticaria, and pruritus. Prevents and relieves nausea and vomiting. Pharmacokinetics ... 

Substituted benzamides include metodopramide (discussed previously) and trimethobenzamide. Their primary mechanism of antiemetic action is believed to be dopamine-receptor blockade. Trimethobenzamide also has weak antihistaminic activity. For prevention and treatment of nausea and vomiting, metodopramide may be given in the relatively high dosage of 10-20 mg orally or intravenously every 6 hours. The usual dose of trimethobenzamide is 250 mg orally, 200 mg rectally, or 200 mg by intramuscular injection. The principal adverse effects of these central dopamine antagonists are extrapyramidal restlessness, dystonias, and parkinsonian symptoms. 

Diphenhydramine (Benadryl) [OTC] [Antihistamine/ Antitussive/Antiemeticj Uses Tx prevent allergic Rxns, motion sickness, potentiate narcotics, sedation, cough suppression, Tx of extrapyramidal (dystonic) Rxns Action Antihistamine, antiemetic Dose Adults. 25-50 mg IV/EM Feds. > 2 y. 2—5 mg/kg IV/EM Caution [B, —] Contra Acute asthma Disp Tabs,... 

A number of the antihistamines, particularly the phenothi-azines and aminoalkyl ethers, have antiemetic actions and thus may be u.seful in the treatment of nausea, vomiting, and motion sickness. Also, those agents that produce pronounced. sedation have application as nonpiescription sleeping aids." - "Several of the phenothiazines have limited u.se in Parkinson-like syndromes as a result of their ability to block central muscarinic receptors." -And. a number of antihistamines, including promethazine, pyrilamine. tri-pelennamine and diphenhydramine, display local anesthetic activity that may be therapeutically useful. ... 

Migraine can often be treated with paracetamol, ibuprofen or aspirin alone, or with combination products containing them. There are also some non-prescription medicines specifically licensed for the treatment of migraine. One such is a coformulation of paracetamol, codeine and the antihistamine buclizine, included for its antiemetic action. Other specific migraine treatments are reviewed below. 

Antihistamines, dronabinol, glucocorticoids, and metoclopramide have antiemetic actions that are useful in the management of vomiting caused by anticancer drugs. Levodopa causes nausea because it is converted to dopamine, which activates dopamine receptors in the emetic center. The answer is (C). 

Antihistaminics are widely used in the palliative treatment in allergic conditions like hay fever, urticaria, some forms of pruritus, rhinitis, conjunctivitis, nasal discharge, mild asthma etc. A few antihistaminics possess potent antiemetic action and hence are frequently employed in the prevention and treatment of irradiation sickness, motion sickness (air, sea, road), nausea in pregnancy and postoperative vomiting. 

Since there was some evidence that these compounds owe their action to interference with the action of histamine, this class has earned the soubriquet "antihistamines." This class of drugs is further characterized by a spectrum of side effects which occur to a greater or lesser degree in various members. These include antispasmodic action, sedative action, analgesia, and antiemetic effects. The side effects of some of these agents are sufficiently pronounced so that the compounds are prescribed for that effect proper. Antihistamines, for example, are used as the sedative-hypnotic component in some over-the-counter sleeping pills. 

Medications for symptomatic relief from vertigo consist of antiemetics, benzodiazepines and antihistamines. They are all mostly aimed at the psychological consequences of dizziness and can all have highly unfavourable side effects, for example, sedation, anticholinergic effects and insomnia. The psychological consequences of dizziness in elderly should rather be treated with information about the condition, supportive help actions and increased social activities, than with drugs. 

Pharmacokinetics Dimenhydrinate has a depressant action on hyperstimulated labyrinthine function. The precise mode of action is not known. The antiemetic effects are believed to be caused by the diphenhydramine, an antihistamine also used as an antiemetic agent. 

Mechanism of Action A phenothiazine that blocks dopamine neurotransmission at postsynaptic dopamine receptor sites. Possesses strong anticholinergic, sedative, and antiemetic effects moderate extrapyramidal effects and slight antihistamine action. Therapeutic Effect Relieves nausea and vomiting improves psychotic conditions controls intractable hiccups and porphyria. 

Dronabinol (Marinof) [C-ll] [Anriemeric, Appetite Stimulant/ Antivertigo] Uses N/V associated w/ CA chemo appetite stimulation Action Antiemetic 4- V center in the medulla Dose Adults Peds. Antiemetic 5-15 mg/m2/dose q4-6h PRN Adults. Appetite stimulant 2.5 mg PO before lunch dinner max 20 mg/d Caution [C, ] Contra Hx schizophrenia, sesame oil hypersensitivity Disp Caps SE Drowsiness, dizziness, anxiety, mood change, hallucinations, depersonalization, orthostatic 4- BP, tach Interactions T Effects W/ anticholinergics, CNS depressants, EtOH 4- effects of theophylline EMS Use caution w/ sympathomimetics, can T hypertension and tach use caution w/ anticholinergics and antihistamines, can T tach concurrent EtOH use can T CNS depression this is a principal psychoactive substance present in marijuana OD May cause extreme psychiatric effects (anxiety, mood changes and depersonalization) keep pt in a quiet environment and provide reassurance activated charcoal may be effective... 

In addition to their well-established antipsychotic properties, the neuroleptics have a number of clinically important properties that include their antiemetic and antinauseant actions, their antihistaminic effects and their ability to potentiate the actions of analgesics and general anaesthetics. 

Several of the older generation antihistamines are used exclusively for situations that do not involve an allergic reaction. For example, some demonstrate significant antiemetic, antimotion sickness, antiparkinsonian, antitussive, and local anesthetic actions (some Hj antagonists are more potent than procaine). They can be found in many OTC products, particularly for the relief of symptoms from the common cold and allergies, as well as by prescription. The effectiveness of the agents in the treatment of motion sickness and Parkinson s disease may be attributed to their anticholinergic actions. 

Hydroxyzine is a piperazine antihistaminic agent that suppresses activity in the subcortical area of the CNS. It has skeletal muscular relaxant properties and exhibits antiemetic, analgesic, and bronchodilating actions. 

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