Tramadaol is an opioid agonist that finds useful in the management of moderate to somewhat severe pain. This drug can be used in combination with other analgesic agents. But it should be carefully used with other centrally active agents as it may lead to serious adverse effects.
Hi everyone today in this video we are going to discuss about tramadol how this drug acts as analysis sake what are the precautions side effects and indications of tramadol what is strike tramadol this is one of the opioid agonists just like the other drugs such as morphine codeine fentanyl tram doll also belongs to the opioid category that’s why this drug is
Used as analysis and particularly this drug is indicated for treatment of moderate to severe pain and whenever this analysis action is required throughout the day then for prolonged analysis action tram doll can be prescribed what is the chemical nature tramdoll is having the structure like this and here you can observe it is not having the steroidal nucleus
But it is a modified structure which is having phenyl ring and cyclohexane ring system which may be compared with the morphine-like structures and just like the morphine tram doll is also having the alcoholic oh group and because this oh group is attached with the cyclohexane now tramdoll can be written as cyclohexanol derivative and this cyclohexanol is having
A side chain at the second position that is nothing but the methyl group so two dash methyl but this methyl group is and at the first portion design the phenyl ring this phenyl ring is having a methoxy group at the third position so now we can write this as 1-3-methoxyphenyl so that is a complete name of the tramadol so tramol is a cyclohexanol derivative
And when we compare this structure with the morphine just like the morphine it’s also having the phenyl ring as well as cyclohexane ring and an alcoholic oh h group is present and because of this structural similarity tramdoll also acts as a opi diagonalist therefore it produces a central analysis now it is the metabolism of tramadol so all we have seen the
Structure of tramadol and here it is having the methyl groups on the nitrogen as well as on the oxygen so these methyl groups can be easily removed during the metabolism such that tram doll can give the nd methyl metabolite or od methyl metabolite so here one of the methyl group is present on the oxygen like methoxy group now this methyl group can be removed
Such that it is going to give a metabolite now this metabolite design the voice group here so this is nothing but oh des methyl tramadol so this is one of the metabolite of tramdoll and this is an active metabolite and highly potent compared to the tramadol this metabolite is around six times more potent than the tramadol so the firm classical effects of this
Drug is because of both parent drug as well as its metabolite odes methyl tramadol so now let’s see how this drug acts this tram dog acts as an agonist on the mu receptors which is response for the central analysis action at the same time this drug can also block the reuptake of the mediators like the norepinephrine and phi hd these two mediators are responsible
For the inhibition of the nosception so by inhibition of their reuptake their levels are going to be increased which increase their inhibitory effect on the noception nonception can be transmitted through the neurons so these nonseptic neurons send the signals through the other neurons towards the higher centers in the brain these nonseptic neurons are going to
Release the non-septum mediators which can act on the post synaptic receptors so when the pain stream is going to be generated in the pre-synaptic neurons they can release these non-septum mediators which can act on the post-synaptic receptors such that the pain signal can be transmitted towards the higher centers of the brain in this way the pain produced at
The periphery can be transmitted towards the brain but here centrally this pain transmission can be controlled by so many other mediators few of the descending inhibitory pathways are present which are going to store the norepinephrine as well as other mediators like phi ht these mediators can act on the presynaptic receptors alpha two receptors so now these
Mediators can bind to this alpha receptors which are inhibitory receptors therefore they can inhibit this pain transmission such that the pain cannot be transmitted towards the higher centers in the brain in this way descending inhibitory pathways can control the nosception but one of the limitation of these descending inhibitory mediators is their reuptake the
Action of these mediators is controlled by their reuptake so these chemical mediators can be re-uptaken into the nerve terminal such that their action is going to be terminated in this way the inhibited reaction of these mediators is controlled by their reuptake now let us see how this tremdoll acts tram doll can act on the non-septic neurons which are equipped
With the new receptors now tramdoll acts as an economist at the mu receptors such that it produces the inhibited reaction on the nonceptor neurons and pain transmission is going to be directly inhibited otherwise tramadol can also act on the reuptake transmitters such that it can inhibit the reuptake of norepinephrine and phi hd so when the reuptake is inhibited
The levels of these mediators are increased which can produce the inhibitory effect on norception in this way tramdoll can produce a direct inhibition on the norception as well as indirect inhibition through elevation of the norepinephrine and firest levels what are the precautions one of the important precaution of tramadol is risk of seizures this risk is even
Observed with a therapeutic dose of tramadol so whenever this drug is prescribed the susceptibility of seizures in the patient should be carefully monitored and particularly this is more important when other drugs are going to be prescribed for example tca is like the amitriptyline and antihistamines like the promethazine which are having the tricyclic structure
And mao inhibitors like phenyl giant triancy prominent and isocarboxy if you have the other opioids like morphine and fentanyl and any other antipsychotics like chloroprompt all these drugs are further increasing the risk of seizures when they are concomptently given along with the tramadol so that’s why this drug should be carefully given with the other centrally
Acting drugs second important precautions are serotonin syndrome this one of the syndrome observed with the elevated levels of serotonin and when the serotonin levels are excessively increased within the central nervous system it can produce few of the symptoms like agitation hallucinations tachycardia hyperthermia and in coordination along with some mental
Confusion all these symptoms are observed with the serotonin syndrome now tramadol can increase the serotonin syndrome and this syndrome is further increased with other drugs like ssris snris tcas and mauve inhibitors which are going to increase the serotonin levels within the cns so again this stamina should be carefully given with all these category of drugs in
Order to prevent the severe serotonin syndrome another important one is the suicidal initiation tramdoll can increase the risk of suicidal initiation and particularly this risk is further enhanced with consumption of alcohol and administration of anti-depressants and tranquilizers all these drugs are going to increase the suicide initiation when they are given
Along with the tramadol similarly another important precaution is the anaphylactic reactions tram doll can produce few of the allergic reactions which is commonly observed with the other opiates so this drug can produce bronchospasm angioedema swelling as well as hives and even a serious condition like the stephen johnson syndrome all these allergic reactions can
Be observed with that tram at all and another important precautions are respiratory depression normally opioids produce a respiratory depression so just like the other opioids stamdal can also produce the respiratory depression which may lead to the respiratory collapse that’s why this drug should be carefully given in the patients who are having the respiratory
Disorders what are the side effects the important side effects include headache nausea warmting and it can also produce some dizziness somnolence and few of the other side effects like constipation dry mouth even display all these side effects can be observed with the tramadol and you can also produce few of the hypersensitive reactions along with the proriders
How it is given tram doll is available as a tablet at a dose of 50 mg even it is available at the other doses and even in combination with the other analysis and it’s also available as a capsule but this capsule is available as an extern release tablet at different doses like 100 mg 200 mg and 300 mg in case of extend release capsule the initial dose is going to
Be started at 100 mg once daily those can be titrated according to the usage but the maximum dose for the external is tablet is 300 mg once daily but the maximum dose for the external is capsule is 300 mg once daily so that’s about this tramadol tramadol is a opioid agonist which is used to treat the moderate to severe pain so whenever this analysis action is
Required throughout the day this tramadol can be given compared with the other opiates the stamidol is having less euphoria but this drug can increase the suicidal initiation even it can prescribe the serotonin syndrome and seizures in the patients just like the other opioids this drug can also produce respiratory depression and anaphylactic reactions this drug
Acts as an on the mu receptors thereby it produces central analgesia as well as it can also inhibit the reuptake of mediators like the fiesta and norepinephrine which are responsible for the inhibition of the nosception and this drug is available as an accident release capsule which is initiated at a dose of 100 mg and the maximum dose is 300 mg so that’s about
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Transcribed from video
Tramadol – Mechanism, side effects, precautions and uses By egpat