Buspirone

hello I'm dr. ken NIDA thanks for watching let's talk about buspirone now this medicine originally came out on the market is busbar but after the patent expired and competition came in the drug company thought they couldn't make any money on it so they stopped making it but this is a good anti-anxiety medicine was first synthesised way back in 1968 the FDA approved it in 1986 and even though the medicine is pretty old it's still among the top hundred medicines prescribed in the United States with more than 8 million prescriptions every year part of the reason it's coming back into vogue is it's not a controlled substance now it's in a class by itself that's unrelated to the benzodiazepines not related to the barbiturates it's not related to other sedatives or anti-anxiety medicines that are out there but it's equally effective for the generalized anxiety disorder maybe if you took some of the benzodiazepine and some people think that it might be a little less effective but it really is quite a good drug and it lacks some of the same side effect profile that the other anti-anxiety drugs have and that's again part of the reason it's coming back into vogue it's primarily used to treat anxiety disorders and specifically the generalized anxiety disorder not so much for social phobia and for panic and obsessive-compulsive disorder and it's not for psychosis and once you start taking the medicine it can take up to four weeks to become totally effective and as with most of these drugs approved only for short-term use even though a lot of people taking for relatively long period of time now if we look at the government's recommendations at the current time the primary therapy for anxiety should be the selective serotonin reuptake inhibitors but there are some problems with those drugs especially coming off of those drugs now if we look specifically at the way buspirone works it has no immediate anti-anxiety effect it has delayed onset of activity so in some individuals might take two weeks or three weeks or four weeks become totally effective it sometimes is used off-label it's off-label in its use in people who have depression it's used with an SSRI with a drug like prozac or celexa or a paxil for people who have unipolar depression or it could be used as an add-on medicine augmentation and people who have what appears to be treatment resistant depression and interestingly it might even be helpful as a sole therapy for treating people with depression but at a higher dose it does about 90 milligrams a day the max under normal circumstances for anxiety would be about 60 milligrams a day but at a higher dose and in combination with other drugs like melatonin it seems that buspirone might actually increase the development increased the growth of nerve cells in the hypothalamus and that's very important because it seems that the antidepressants work by increasing neurogenesis if it doesn't increase neurogenesis it's not going to work as an antidepressant apparently well it also might be helpful for women who suffer from the hypoactive sexual desire disorder if indeed that's a legitimate disorder but it's helpful for that and it might be helpful as an add-on and people who have schizophrenia well in other individuals people who have irritability or aggression or agitation associated with either dementia or with mental impairment maybe in a nursing home or elsewhere seems to be equally effective to Haldol for the agitation and better than Haldol for the tension and the anxiety Haldol is used much too often ly much too often has a lot of side effects so if possible it's good idea to consider a relatively safe for drug it's also used for irritability due to autism and in Japanese studies it's been found to be equivalent in its activity to Ritalin in the treatment of attention deficit hyperactivity disorder or ADHD seems to be as good as but not better than strattera and Ritalin some of the other drugs well it seems that it's not effective in therapy of withdrawal reactions that people have after they try to stop the benzodiazepines are stopped the barbiturates or for treatment of the alcohol DTS well it might be helpful in people who are taking an SSRI who suffer from either sexual dysfunction which isn't uncommon with the SSRIs or who have jaw pain or jaw spasm from the SSRIs it has no benefit when you take the bus prone in helping you discontinue either cigarette smoking or alcohol or cocaine or THC but it's okay to use in people who have anxiety if they're dependent on alcohol but it's probably a good idea to stay away from it if people are dependent on opioids now what is generalized anxiety disorder well you have to realize that the pill is so old that it was brought out under the DSM 3 that's the American Psychiatric Association classification of diseases well it was under the third edition so what is generalized anxiety disorder in the third edition of this American Psychiatric Association Journal or volume or book well you have to have in order to qualify at least one month of three of four symptoms and the symptoms have a lot of subgroups so one would be vigilance and scanning in the vigilance of scanning group symptoms would be distractibility or difficulty concentrating or insomnia or feeling like you're on edge or irritable or suffer from erectile dysfunction second group would be apprehensive expectations anxiety and worry and fear rumination or anticipation of misfortune either to yourself or to someone else the third group would be autonomic nervous system hyperactivity so those symptoms would be sweating and your heart pounding cold clammy skin dry mouth lightheadedness paresthesias tingling and numbness of your fingers and your toes and upset stomach and feeling hot and cold and going to the bathroom frequently either to urinate or defecate or flushing or power having increased heart rate or increased respiratory rate and the fourth category would be motor tensions people who feel shaky or jittery or restless err jumpy or have easi startled or tremble or have tension or muscle aches or inability to relax or maybe the eyelid is twitching a little bit or the brow is furrowed well that's part of the reason that we have such a major problem with psychiatric diseases because the classification of the diseases doesn't make any sense those are just symptoms that happen to be lumped together but they're not specific but that's what constitutes the generalized anxiety disorder at least under which the buspirone was brought to market now does the drug have some side effects yeah it has some side effects fortunately very mild very few in number so the standard would be nausea and headache and some dizziness and trouble concentrating and maybe a little bit of nervousness and the numbness and the tingling and the abnormal dreams and the a taxi and the excitedness but those tend not to be much of a deal little bit more important but very rare would be hallucinations or the serotonin syndrome or even some seizures but many of the side effects resolve even though the and continues to take the medicine even at a higher dose seems the West Peron has minimal sexual side-effects and again might be used in treatment of some of the side effects sexual side-effects due to the SSRIs it's less sedating than some of the other anti-anxiety medicines no significant functional impairment with the drugs but anytime you take a drug that does act on the central nervous system the effects can be unpredictable so you need to have or need to exercise extreme caution when you start taking the drug to see how it works on you is it safe for you to drive motor vehicle if not then shortly thereafter you'll be able to drive well it doesn't seem to increase the alcohol induced impairment this continuation rate of people who stopped the medicine because of a side effect it's about 10% after about a month and that's even before the medicine has become fully effective so some of the symptoms might actually be the generalized anxiety disorder that hasn't been completely controlled yet the dizziness insomnia nervousness and drowsiness and lightheadedness and some of the gastrointestinal problems well interestingly with this medicine food can decrease the metabolism in the liver so it can actually increase the amount of the drug that's in your system so it increases what we call the area under the curve the amount of drug in your system for a 24-hour period by about 85% and increases the peak concentration by almost twofold it's interesting that the food seems to decrease the absorption but wow it's decreasing the absorption it also has a greater effect on decreasing the metabolism in the liver so overall it increases the bioavailability of the drug so that means that you can take the drug either with food or without food but you have to do it consistently either with the food or without the food because otherwise you're going to have varied amount of medicine in your system now if you're going to take buspirone and you're already taking some of the other sedatives or hypnotics it's a good idea to stop taking those before you take the drug and the reason is because on some of the drugs like benzodiazepines you're likely to have some withdrawal reactions irritability anxiety agitation insomnia tremor abdominal cramps are vomiting sometimes you have seizures are sweating well if you start taking the drug like West Berlin it's not gonna stop any of those side effects from withdrawing from the benzodiazepines but you won't know if some of those side effects happen to be from the buspirone so you're in effect get rid of the benzodiazepines the other tranquilizers before you start taking the medicine when you start taking the medicine a good dose to start with would be 15 milligrams a day you break that up into either two or three segments either seven and a half twice a day or five milligrams three times a day increase it every three days or so you can increase to a maximum daily dose of left 60 milligrams typically it's 20 milligrams twice a day 30 I'm sorry 20 milligrams twice or three times a day or thirty milligrams twice a day the tablets are divided quite conveniently so you can either divide them in half or divide them in third so it means if you have a 30 milligram tablet you could divide it into three tens or two 15s or a twenty and a ten if we talk about the pediatric population people between the ages of 6 and 17 well people argue whether the drug is appropriate it's off-label it's not been approved for the pediatric population but certainly of those 5 milligrams a day seems to be quite easily tolerated as a matter of fact people argue whether the maximum dose in the pediatric population should be 20 milligrams or 60 milligrams as it is in adults well the good news is that it's not associated with sedation it's not associated with cognitive impairment or psychomotor impairment not associated with euphoria it's not a muscle relaxant it's not an anticonvulsant and that means this is not a drug of abuse so during pregnancy it's probably safe it's okay definitely in animals hasn't been tested in humans breastfeeding again it's not studied it's not recommended but there doesn't seem to be any specific harm that we know of pediatric population as I mentioned it's been studied at doses of seven and a half milligrams twice a day all the way up to 30 milligrams twice a day this is not a drug that's going to kill you the lethal dose been test animals is somewhere between a hundred sixty and five hundred fifty times the recommended dose in humans so they gave the drug to volunteers and they gave them an overdose the maximum dose of 60 milligrams so they gave him 375 milligrams and all that happened in otherwise healthy male volunteers was they had some nausea and vomiting and dizziness and drowsiness the pupils constricted and they had some upset stomach even when taking it a dose of 2400 milligrams no you get us some restlessness and some tremor and some muscle rigidity there's only one death that's been reported from an overdose of buspirone and that was a dose of 450 milligrams but the person was also taking alprazolam xanax alcohol cocaine and taking a heart medicine well the contraindication the reason you shouldn't take the medicine is if you have metabolic acidosis in other words uncontrolled diabetes out of control if you're taking an MAO inhibitor not a good idea certainly can have major problems if you have severe liver or kidney impairment don't take the drug and certainly if you've had the medicine before and you had an allergic reaction to it not a good idea interestingly just to go back for a moment as mentioned before a low dose of buspirone 15 milligrams a day in combination with three milligrams of melatonin every day might stimulate neurogenesis specifically in the hippocampus and it appears that depression is associated with decline in the volume of the hippocampus and the antidepressants work to increase the hippocampal neurogenesis so as I mentioned it might be a therapy perhaps somewhat higher doses for people who have depression the way the drug works well it's an agonist of serotonin specifically serotonin the 5-ht one a receptor and it might also push up the levels of oxytocin and that's relatively good it's postulated that it increases the serotonin in the amygdala and other of the Centers of the brain that deal with anxiety but it seems to have less effect on other serotonin receptors so there's other 5ht 1b 1c and there's HT 2 whatever else it also seems to alter the dopamine metabolism so it seems that it can at least in part work to cause some hypo activity which is a problem for people who are anxious and moving about and restless so that's a good reaction can decrease some of the stereotypic activities that people have doesn't block the catalepsy it seems that it's a partial agonist of the alpha-1 adrenergic receptors in other words works like norepinephrine but it's very weak probably relatively clinically unimportant for most people but in some people might lead to a little bit of restlessness that might be to do with the newer adrenalin norepinephrine or the dopamine originally when it came out it was thought that would ease this drug might lead to some part i've dyskinesia some of those peculiar movements you get with the antipsychotic drugs used to treat either schizophrenia or the mania of manic depressive disorder maybe lead to restlessness or some dystonia that never fortunately turned out to be the case well it doesn't interact with the GABA a receptor that's where the benzodiazepines work it's not an anticholinergic not an antihistamine not an imp not a muscle relaxant seems that it is broken down into some metabolites one is called 1pp that's actually at a higher concentration than the buspirone itself but it has some potent activity it seems to act to stimulate the noradrenaline but the effect probably is more in animals than it is in humans the bioavailability of the medicine is relatively low if we look at the pill form it's only ninety percent as effective or at least the bioavailable as the solution form it has relatively low bioavailability in the system because of the first pass metabolism by the liver so you take it it gets absorbed from the intestine goes right to the liver and is metabolized so that means the bioavailability is only four percent of what it would be if we gave it to a person intravenously so after 40 to 90 minutes of the 20 milligram dose there's almost undetectable amount in the system the amount is relatively low and it varies significantly between the individuals and the half-life of the medicine is only about an hour to an hour and a half but the half-life I'm sorry the peak concentration is about hour to an hour and a half and the half-life of the drug is somewhere between 2 and 11 hours but it could be up to as long as 33 hours and some individuals now it's metabolized by the liver as I mentioned and when it's metabolized it's metabolized to a chemical that is known as 6 hydroxy buspirone and that seems to have high affinity for the same areas that the buspirone acts in and as a matter of fact it has an important role in to therapeutic activity of the drug and it's present in an amount 40 times greater than the buspirone in the system the 1pp is present about 20 fold greater than it is in the than the buspirone but the question is how relevant is that we're not quite sure at this time now it seems that about 30 to 60 percent is going to be excreted in the urine about 20 to 40 percent is going out in the feces but 90 percent is going to be bound to the different proteins in the system it doesn't displace anything else that happens to be on the protein so it's not going to change the concentration of by lanten or warfarin or propranolol but it may displace the digoxin if you happen to be taking digitalis type preparations now there's a problem if you happen to be taking some other drugs so if you take it to a con is all it's going to increase the amount of buspirone by about 19 fold if you're taking sirs only antidepressant it's gonna increase the amount of buspirone by about 50 fold so classes potentially and grapefruit juice increases about fourfold on the other hand if you happen to be taking rifampin it's going to decrease the amount of buspirone in the system by that 90 percent significant problem also if you're taking tegretol or carbamazepine doesn't seem to have too much effect on some of the other drugs but you do have to be very cautious if you're taking verapamil or rifra Meissen or del pi azam there's no change however if you're taking a me trip Deline nortriptyline might have a little tiny effect if you're taking the valium but that's relatively minimal effect and we don't worry about it we don't worry about the ibuprofen or does it for me nor other kinds of drugs you can take the sleeping pills if you happen to be taking down Maine or if you're taking halcyon it's okay but you shouldn't take it within 14 days of a MAO inhibitor if you take it within 14 days of MAO inhibitor you might have a horrible reaction that we call a serotonin syndrome and that's associated with gastro gastrointestinal and neurologic and autonomic nervous system activity change in your mental status you're agitated you have tremor you perspire a lot you have diarrhea and dry mouth and muscle rigidity all sorts of problems metabolized about the same in young people and older people but if you have liver Pearman it's going to increase the amount in the system by about three fold up to 14 fold and if you have significant kidney failure it's not a good idea actually even if you have my adrenal failure mild renal disease it's going to increase the concentration in the system by about fourfold and interestingly if you happen to be evaluated for a relatively unusual condition a tumor of gland called a pheochromocytoma well this drug the buspirone might actually give a false positive result so you should be off the bus prone for about 48 hours about two days before you're tested for a pheochromocytoma pheochromocytoma increased nervousness increase blood pressure increased heart rate so some of the same kind of symptoms that you might get in generalized anxiety disorder the good news about the drug is it's not carcinogenic not mutagenic you don't develop dependence or tolerance as a matter of fact if the drug is given to people who use recreational drugs or drink alcohol to excess actually they don't have any preference between buspirone and a placebo so that means there's no abuse no diversion of the drug no drug seeking behavior drug was first synthesized by a drug company known as me Johnson way back in 1968 patented in 1975 originally it was thought that it might be an anti-psychotic activity or might die psychotic drug because of the activity on the dopamine receptors but it was ineffective for that purpose so it was repurposed as an anti-anxiety drug and bristol-myers Squibb sought FDA approval for that purpose generalized anxiety disorder patent expired in 2001 and due to the competition and due to the low price they figured they couldn't make any money on it so they stopped making it so now it's available only as a generic but wouldn't you know it for a while in 2019 milan laboratories had a shortage of the drug that was being manufactured at their Morgantown plant in Virginia the cost of the medicine that's good news the cost of this medicine is very low considering its good activity for cash you could buy 10 milligram pill 60 of them cash 14 to $20 you have a coupon from good rx you go over to Walmart it's about $4 CVS it's $16 Walgreen more than $19 and if you want the 30 milligram pills you can get 60 of them again for cash 30 to $40 except CVS and Walgreens it's more than $60 and if you have a coupon mmm it's $14 except CVS and Walgreens for some reason they're always relatively high 35 or 40 dollars those drugstores well anyway that's the story of buspirone it's a relatively good drug for treating anxiety generally not associated with significant side-effects not associated with abuse or dependence and it's enjoying the Renaissance principally because the country now seems to be moving away from the benzodiazepines moving away at least for a while treating the anxiety disorders with the selective serotonin reuptake inhibitors it seems that unlike the benzodiazepines this drug doesn't work nearly as quickly so you can't take it on an as-needed basis because remember it's gonna take anywhere between two and four weeks to become totally effective so I hope you enjoyed the show thank you for watching if you enjoyed maybe a tell a friend may be a concern consider subscribing to the show and certainly we appreciate your interest I'm dr. ken landau [Music]

Channel: wellnowdoctor

Views: 50,042

Rating: 4.9285135 out of 5

Keywords: Buspirone, Buspar, anxiety, benzodiazepam, xanax, lorazepam, valium, ADHD, sexual dysfunction, melatonin, depression

Id: zRpAwicLWwI

Length: 25min 55sec (1555 seconds)

Published: Thu Dec 12 2019