2.1 Drug Profile of Baclofen
Synonym : Lioresal, Kemstro
Molecular Formula : C10H12ClNO2
Structure :
Chemical name : 4-amino-3-(4-chlorophenyl)-butanoic acid
Molecular weight : 213.661 g/mol
Description : White to off-white
Solubility : Slightly soluble in water, Very slightly soluble in methanol,
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Pka : 4.00
Category : Skeletal muscle relaxant
Mechanism of action : Baclofen is a derivative of gamma amino butyric acid (GABA) which is naturally occurring neurotransmitter. It produces its effect by activating GABAB receptor. It is used in the treatment of spasticity. Pharmacokinetic
| 1. corticosteroid 2. bronchodilator 3. ACE inhibitor4. cholesterol 5. benzodiazepine 6. potassium sparing diuretic
Gabapentin modulates the action of glutamate decarboxylase (GAD) and branched chain aminotransferase (BCAT), two enzymes involved in GABA biosynthesis and it had shown no interaction with the sodium or L-type calcium ion channels
This paper will illustrate several aspects of how drugs affect our lives. Addiction philosophies including the psychology and physiology will be explained in an attempt to describe how drugs affect our bodies both physically and mentally. Secondly, different drug categories types will be covered including: stimulants, depressants, narcotics, hallucinogens, and cannabis. Each of these categories has different addiction potentials and effect levels including withdrawal symptoms. Finally, the abuse of prescription drugs and their effects will be discussed.
Mechanics of action: The mechanics of the actions for this drug is to relax the muscles around your airways.
These are ligand gated chloride-selective ion channels that become activated by GABA. The binding of the previously stated substances increases the binding of GABA, this has the effect of increasing the total transport of chloride ions across the cell membrane of the neuron. The increase in chloride ions within the neuron, hyperpolarizing the membrane potential. Therefore, the difference in resting potential and threshold potential is increased, this causes firing to be less likely. This decreases the chances of firing within the neurons. Causing the desired outcomes, such as initiate sleep and a calming effect (Tan et al., 2011). Diazepam can cause such outcomes in two ways, the first by increasing the binding ability of GABA to activate the receptor and the second by increasing the chance of chloride channel opening as a response to GABA binding. Secobarbital sodium is similar due to producing the same effects as diazepam at lower concentrations but when the concentration rises. Secobarbital sodium directly activates the GABA receptor. This suggests two binding sites which are specific to barbiturates. This explains the higher 96 hour LD50 values compared to diazepam (Makkar et
Thank you for sharing your clinical experience regarding the adverse effect of baclofen on your patient associated with physical therapy treatment. I have multiple negative experiences regarding the side effects of oral muscle relaxants drugs as well as with my colleagues from work.
The rat phrenic nerve preparation is very useful as it teaches us not only a lot about neuro muscular and muscle physiology but also the pharmacodynamics of different drugs such as neuromuscular blocking agents and determining their potency at blocking the neuromuscular junction. This preparation was originally used for the bioassay of tubocurarine (Bülbring et al, 1997). However there are a few limitations to this prep, for example it is hard to differentiate between the different neuromuscular blockers, whether they are depolarizers or non-depolarizers because depolarizers fail to reverse the effects of non-depolarizers. As a result of this, another prep is preferred namely the chick sciatic nerve-tibialis anticus muscle (Vogel, 2013).
Baclofen is one of the many muscle relaxers, it helps with muscle spasms and tightness. It helps in treating stabbing nervous pain and sclerosis It is available as a tablet that can be taken by children as young as 12 years old. Side effects include nausea, vomiting, confusion, drowsiness, headache and muscle weakness. It is ranked A in the FDA’s A through X pregnancy safety for making medicines, A being
Due to their safety and improved effectiveness, they have largely replaced barbiturates as drugs of choice in the treatment of anxiety. They also have hypnotic, anticonvulsant and muscle-relaxing activities, but do not exhibit analgesic action or antipsychotic activity. The representatives of this group are:
antagonists play two important roles in muscle function: (1) they maintain body or limb position, such as holding the arm out or standing erect; and (2) they control rapid movement
The compound already presented an interesting in vitro activity in its initial tests and currently is thought to be one of the most active benzothiadiazine-derived AMPA-PAMs reported []. Further conducted intracerebral microdialysis experiments allowed detection of micromolar concetration of 1 in mouse nucleus accumbens (NAc) dialysates. It means that the compound is able to cross blood-brain barrier (BBB) after intraperitoneal injection (ip) (see section paragraph). Intracerebral microdialysis is a known experiment that can be applied to evaluate in vivo compound’s p pharmacokinetic (PK) and pharmacodynamic (PD) profile. Nevertheless, it is crucial the compound remains in the specific brain of interest for a sufficient time and at the appropriate to evoke its function and achieve the desired effect. Therefore, examination in vivo of the novel compounds stability plays pivotal role here. In fact, chemical degradation of compound can lower its sufficient concentration below the therapeutic dose. Moreover, as explained in detail in introductory paragraphs, the AMPA-PAM activity usually resides only in one enantiomer
Medications , which may be used to treat muscle problems and other symptoms. Drugs such as diazepam, baclofen, and dantrolene are sometimes used to control muscle spasticity. Anticholinergic drugs may be used to help control abnormal movements. Alcohol or Botox injections into muscle may be used to reduce spasticity for a short time so health care providers can work to lengthen a muscle. Baclofen infused into the spinal canal under control of an electronic pump may be used to control spasticity for long periods of time. Other drugs may also be given to control seizures.
GHB was first synthesized about thirty years ago by Dr. H. Laborit. He was a French researcher interested in exploring the effects of GABA (gamma-aminobutyric acid) in the brain. Over the years many researchers have studied GHB’s effects. In Europe it is used as a general anesthetic, a treatment for insomnia and
For task one, we are required to find eight straight chain 1-monochloroalkanes, eight 1-alchohols, and eight 1-monofluoroalkanes. Many online databases list compounds like these and report specific or averaged scientific data. For example, PubChem, NIST, and Chemspider all have reputable data with sources listed for each data point. Following the assignment formatting guidelines, I will construct a table the 24 compounds
There are two types of muscle relaxants. First, is the antispastic agents that are not recommended for low back pain treatment because it carry indication for spasticity related to injury at the central nervous system. Second, the muscle relaxants is antispasmodic agents that can be used as treatment plan for low back pain if patients do not respond sufficient to first-line analgesics. It should be used only for short time period, if possible no more than 2 weeks in total. Muscle relaxants show better results in reducing pain and relieving symptoms, but it is less effective than NSAIDs. It also can cause more side effects if the patients used it. The major side effects related with muscle relaxants are linked with the central nervous system,