Sedation side-effects

The sedation side effect commonly observed on administration of classical antihistaminic drugs has been attributed in part to the ease with which many of these compounds cross the blood brain barrier. There have been developed recently a series of agoits, for example, terfenadine (198), which cause reduced sedation by virtue of decreased penetration into the CNS. This is achieved by making them more hydrophilic. Synthesis of a related compound, ebastine (197),... 

Drug Chemical Classification Equivalent Oral Dose (mg) Sedation Side Effects Autonomic Extrapyramidal Reactions ... 

The side-effect profile of duloxetine is similar to that of SSRIs. Like the SSRIs, duloxetine does not affect cardiac conduction or lower the seizure threshold. In most patients, duloxetine is not associated with sedation. Side effects that differ from those of SSRIs are hypothesized to be related to the increased noradrenergic activity of this drug and include dry mouth, constipation, and increased sweating. 

Because any opiate derivative will suffice to soothe heroin cravings associated with withdrawal, methadone, a synthetic opiate that has no sedating side effects, has been an effective treatment for heroin and morphine addiction for more than 30 years. The medication is taken orally and suppresses narcotic withdrawal for a period of 24 to 36 hours. Methadone can be taken continuously for 10 years or longer with no harmful side effects. 

Slow dose titration may delay onset of therapeutic action but enhance tolerability to sedating side effects... 

For sedating side effects at high doses, lower the dose... 

Adverse Effects. Patieut acceptauce of beuzodiazepines usually is not a problem, and except for sedation, side effects are reported... 

Figure 19.19 Compounds related to the antihistamine arena. Compound 41, diphenhydramine (Benadryl ) is an older antihistamine that exhibits considerable sedating side-effects. Analogs 42 to 44 (fexofenadine (Allegra ), loratadine (Claritin ), cetirizine (Zyrtec ), respectively) are newer, nonsedating antihistamines. Many of the newer agents are now thought to be good substrates for P-glycoprotein (Pgp), which is situated within the BBB and serves to pump drugs out of the CNS and into the cerebral circulation (brain capillaries).

Duloxetine 60 mg 60 mg For depression, GAD neuropathic pain and incontinence (see BNF) Mane if insomnia, nocte if sedation side effects GAD - start at 30mg max 120mg... 

Benzodiazepines. Several BZs have anticonvulsant activity and ate used for the treatment of epilepsy producing their anticonvulsant actions via interactions with the GABA /BZ receptor complex to enhance inhibitory GABAergic transmission (1). The anticonvulsant actions of the BZs tend to tolerate upon chronic usage in six months, and BZs also lead to withdrawal symptomatology. Other side effects include sedation, ataxia, and cognitive impairment. 

The side effects or toxic effects that the calcium antagonists have in common are hypotension, facial flushing, headache, di22iness, weakness, sedation, skin rash, edema, constipation, and abdominal discomfort (nausea, vomiting, and epigastric pressure). 

Methyldopa is effective in mild, moderate, and severe hypertension but a thiazide-type diuretic is needed to overcome the fluid retaining side effect. Methyldopa has been shown to prevent and induce regression of ventricular hypertrophy in hypertensive patients. The principal side effects are sedation, drowsiness, nasal congestion, fluid retention, and in rare occasions, hemolytic anemia. 

When clonidine is withdrawn abmpdy, patients may experience a rebound hypertensive phenomenon, whereia blood pressure rises rapidly to a level higher than the predmg level. These patients may experience symptoms of headache, tachycardia, agitation, and nervousness. If rebound hypertension occurs, resumption of clonidine therapy or adrninistration of phentolamine reduces the blood pressure. For clonidine withdrawal, the dose should be reduced gradually over a two-week period. The principal side effects are sedation, dry mouth, drowsiaess, di22iQess, and fatigue. 

Guanfacine. Guanfaciae, used ia patients having mild to moderate hypertension, can lower blood pressure 50/25 mm Hg (systoHc/diastoHc) ia hypertensive patients. Side effects such as sedation, dry mouth, and asthenia are less as compared to those of guanaben2 and clonidine. Guanfaciae reduces blood cholesterol and triglyceride and does not cause glucose iatolerance. 

Rilmenidine. RiLmenidine is a central a2 adrenoceptor agonist and has been shown to be a potent centrally acting antihypertensive agent without the prominent side effect of sedation. 

Opioid drugs are often more effective than other nonnarcotic treatments, but they are also associated with more side effects making them less suitable for many patients. Higher doses which are more effective are also associated with undesirable effects such as sedation. 

They act as analgesics by inhibiting release of nociceptive neurotransmitters from primary afferent terminals as well as by depressing post-synaptic potentials on second order neurons. Opioid receptors are also present on some nociceptors and their expression and peripheral transport is increased upon peripheral inflammation. Peripheral opioid analgesia has been established in animal models. Although clinical studies have yielded mixed results so far, this field holds great promise. Despite side effects, such as euphoria, dysphoria, sedation, respiratory depression and obstipation and tolerance and dependence phenomena which arise upon... 

The drug was subsequently reintroduced for treatment-resistant or treatment-intolerant patients in the UK and USA in 1990. The drug is completely free of extrapyramidal side effects but has to be monitored for the development of neutropenia and agranulocytosis. Other problems include sialorrhoea, sedation, reduction in seizure... 

As sedation is one of the major side effects associated with antihistamines, the test compounds were also evaluated for their sedative potentials. This was determined by measuring the reduction in locomotor activity using an ac-tophotometer [6,7]. The test compounds and the reference standards (chlorpheniramine maleate and cetirizine) were administrated orally at a dose of 5 mg/kg in 1% CMC. 

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