Gastrointestinal Pharmacology II: Pharmacologic Management of Nausea and Vomitin
Terms
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Antiemetic Agents - Single-Use Agents includes:
1.
2.
3.
4.
5. -
Antiemetic Agents - Single-Use Agents includes:
1. Phenothiazines: Chlorpromazine (Thorazine)
Perphenazine (Trilafon)
Prochlorperazine (Compazine)
Promethazine (Phenergan)
Thiethylperazine (Torecan)
2. Droperidol (Inapsine)
3.Metoclopramide (Reglan)
4. 5-HT3 Antagonists: Granisetrol (Kytril), Palonosetron (aloxi), Alosetron (Lotronex), Ondansetron (Zofran), Dolasetron (Anzemet)
5. Antihistamine Agents: Cyclizine (Marezine), Meclizine (Antivert), Diphenhydramine (Benadryl), Dimenhydrinate (Dramamine), Hydroxyzine (Atarax);
Anticholinergic Agents: Trimethobenzamide (Tigan),
Scopolamine (Transderm-Scop) -
Phenothiazines
mechanism of action: -
Phenothiazines
mechanism of action: inhibit dopaine receptors centrally in the CTZ, and peripherally blocks VAGUS NERVE in the GI tract -
Phenothiazines
clincal uses: -
Phenothiazines
clincal uses: TREATMENT of nn/v induced by mildy emetogenic chemotherapy; PREVENTION of n/v secondary to anesthesia, radiation, cancer, drug toxicity and other nauseating stimuli -
Phenothiazines
adverse effects: -
Phenothiazines
adverse effects:
1. EXTRAPYRAMIDAL SYMPTOMS (EPS): dystonia, akathisia, tardive dyskinesia
2. anticholinergic
3. cardiovascular: HYPOTENSION
4. CNS: sedation
5. hyspersensitivity: skin rash -
Phenothiazines
cautions and considerations: -
Phenothiazines
cautions and considerations:
1. contraindications: severe cardiovascular disease, severe CNS depression
2. pediatrics: increased likelihood of EPS; increased risk of hepatotoxicity
3. elderly: increased likelihood of EPS, hypotensive, anticholinergic, and sedative effects
4. Parkinson's disease: potentiation of EPS
5. pregnancy: not recommended
6. lactation: excreted in breast milk -
Phenothiazines
drug interactions: -
Phenothiazines
drug interactions:
1. CNS depressants
2. medications with anticholinergic effects
3. medications that cause EPS
4. hypotension-producing medications -
Droperidol (Inapsine)
mechanism of action: -
Droperidol (Inapsine)
mechanism of action: blocks domanine receptors in the CTZ -
Droperidol (Inapsine)
clinical uses: -
Droperidol (Inapsine)
clinical uses: antiemetic during SURGICAL and DIAGNOSTIC procedures; single-agent therapy or in combination with other antiemetics for prevention of CHEMOTHERAPY INDUCED n/v -
Droperidol (Inapsine)
adverse effects: -
Droperidol (Inapsine)
adverse effects:
1. EPS
2. cardiovascular: hypotension (mild-moderate); tachycardia
3. CNS: sedation, drowsiness, dysphoria, anxiety
4. respiratory depression: when used with narcotic analgesic -
Metaclopramide (Reglan)
mechanism of action: -
Metaclopramide (Reglan)
mechanism of action: inhibit dopamine receptors centrally in CTZ and peripherally in the GI tract; accelerates gastric emptying -
Metaclopramide (Reglan)
clincal uses: -
Metaclopramide (Reglan)
clincal uses: single-agent or in combination with other antiemetics for prevention of cancer chemotherapy-induced and postoperative n/v; treatment of drug-related postoperative n/v -
Metaclopramide (Reglan)
adverse effects: -
Metaclopramide (Reglan)
adverse effects:
1. EPS: WORSENS Parkinsonian symptoms, seizures
2. CNS: drowsiness, sedation, agitation
3. CV: hypotension, hypertension
4. GI: diarrhea, nausea -
5-HT3 Antagonists
mechanism of action: -
5-HT3 Antagonists
mechanism of action: BLOCKS the neurotransmitter SEROTONIN, 5-HT3 receptors in the cut, CTZ and VC in the GI tract and centrally in the CTZ -
5-HT3 Antagonists
clinical indications: -
5-HT3 Antagonists
clinical indications: prevention of n/v associated with intial and repeat courses of EMETOGENIC CANCER CHEMOTHERAPY (including cisplatin), prevention/treatment of post-operative n/v -
Antihistamine/Anticholinergic Angents
mechanism of action: -
Antihistamine/Anticholinergic Angents
mechanism of action: BLOCK ACETYLCHOLINE RECEPTORS in the VC and vestibular center; reduce vestibular stimulation and labyrinthine function -
Antihistamine/Anticholinergic Angents
clinical indications: -
Antihistamine/Anticholinergic Angents
clinical indications:
1. prevention and treatment of n/v and dizziness of motion sickness
2. hydroxyzine (Atarax) administered IM pre-and postoperatively to control vomiting
3. diphenhydramine (Dramamine) used as an adjunct in combination antiemetic regimens to provide mild drowsiness and protect acgainst EPS of some drugs
4. trimethobenzamide (Tigan) used for general n/v -
Antihistamine/Anticholinergic Angents
cautions and considerations: -
Antihistamine/Anticholinergic Angents
cautions and considerations:
1. pregnancy, breast-feeding, pediatric, elderly: usen ot recommended
2. actute asthma, predisposition to urinary retention, obstructive disease of GI/GU tract, prostatic hypertrophy, glaucoma. -
Antiemetic Agents - Adjunctive Agents for Chemo-Induced N/V includes:
1.
2.
3.
4. -
Antiemetic Agents - Adjunctive Agents for Chemo-Induced N/V includes:
1. Unknown
-Corticosteroids
-Dexamethasone (Decadron)
-Methylprednisolone (Solu-Medrol)
2. Bensodiazepines (* end in "pam")
-Lorazepam (Ativan)
-Diazepam (Valium)
3. Cannabinoids
-Dronabinol (Marinol)
-Nabilone (Cesamet)
4. Substance P/Neurokinin 1 Receptor antagonist
-Aprepitant (Emend) -
General Guidelines for Antiemetic Therapy - Non-pharmacologic:
1.
2.
3. -
General Guidelines for Antiemetic Therapy - Non-pharmacologic:
1. Dietary Modification/Changes
2. Stable physical positions
3. Behavior Modification -
General Guidelines for Antiemetic Therapy - Pharmacologic:
1.
2.
3. -
General Guidelines for Antiemetic Therapy - Pharmacologic:
1. Simple, Uncomplicated N/V
a. minimal therapy
b. SINGLE-AGENT therapy preferred
2. Complex N/V
a. two or more antiemetics often required
b. small to moderate dosage regimens
3. Cancer Chemotherapy-Induced N/V
a. combination therapy
b. antiemetic therapy most effective when used as a PROPHYLAXIS
c. EPS usually controlled with ANTI-PARKINSONION DRUGS (benztropine, trihexyphenidyl), anticholinergic agent (atropine) or diphenhydramine
d. anticipatory N/V - use bensodiazepines (lorazepam) helpful - Caution with CNS adverse effects