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leebird-simmer · 2 years

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All About: Opioids

- Opioids are substances that act on opioid receptors to produce morphine-like effects.

- Opioids include opiates, an older term that refers to the drugs derived from opium, including morphine.

Opioids = Narcotic Analgesics

- The opioid drugs are narcotic analgesics:

sleep-inducing (narcotic)

pain-relieving (analgesic)

- They are the best painkillers known to humankind, and they also produce a sense of euphoria.

- They create a sense of relaxation, but at high doses, they can lead to coma and death.

Opium

- Opium has been used recreationally and in medicine for thousands of years (since 5000 BC in China).

- Opium is an extract of the poppy plant (Papaver somniferum).

- Opium is prepared by drying and powdering the milky juice taken from the seed capsules of the opium poppy just before ripening.

- Opium contains morphine, codeine, thebaine, narcotine, and other ingredients.

- Recreational users often smoke opium for its rapid absorption from the lungs.

Opium-Based Products

- Laudanum, an opium-based medicinal drink, was introduced to England in 1680.

- Drinking laudanum-laced wine was the accepted form of opium use in Victorian England & USA.

- Up to the 20th century, laudanum was common in popular remedies.

Morphine

- extracted from the poppy plant in 1805 by a German chemist named Friedrich Serturner

- It was the first time an active ingredient of any medicinal plant was isolated.

- Extraction of morphine allowed doctors to prescribe it in known dosages.

- very powerful analgesic and euphoric drug

- named after Morpheus, the Greek god of dreams

Codeine

- isolated in 1832

- less analgesic effect and fewer side effects than morphine

- A potent cough suppressant, it is often included in cough medicine and in pain relievers.

Heroin

- was developed by the Bayer Company in 1874 to be more effective in relieving pain and cough without the danger of addiction.

- Heroin was made by adding two acetyl groups to morphine, making it more lipid soluble. The very rapid action of heroin is responsible for the dramatic euphoric effects achieved with that drug.

- as a street drug, preferred over morphine

- pharmacological effects of morphine and heroin are essentially identical because heroin is converted to morphine in the brain.

Oxycodone

- semisynthetic opioid derived from thebaine

- In 1916, German scientists at the University of Frankfurt developed oxycodone as an analgesic less addictive than morphine.

- Oxycodone was approved by the FDA in 1950 as Percodan (mix of oxycodone & aspirin).

- Since the early 1960s, abuse of prescription opioids containing oxycodone has been a major concern in the USA.

- In 1996, Purdue Pharma introduced (and aggressively marketed) OxyContin, a controlled release formulation of oxycodone.

- Purdue advertised Oxycontin as non-addictive because the drug was designed to be released within the body over a 12-hour period.

- Recreational drug users quickly learned to get high by crushing or dissolving these time-release pills.

- Spread of Oxycontin abuse has resulted in increased deaths from overdose.

Molecular structure of morphine, codeine, heroin, and naloxone

Selected natural and synthetic opioid drugs

Heroin = Schedule I

Morphine, oxycodone, fentanyl, opium, methadone = Schedule II

Opioids: Routes of Administration

- Recreational users often smoke opium for its rapid absorption from the lungs.

- Morphine:

in hospitals: intravenous, intramuscular, or subcutaneous injection; or given orally

in the streets: inhalation

- Oxycodone, vicodine: taken orally as pills

- “Snorting” heroin leads to rapid absorption through the nasal mucosa. Subcutaneous administration (”skin popping”) may precede the more dangerous “mainlining” (IV injection).

Opioids: Distribution

- Morphine and oxycodone have similar fat-solubility and only a small fraction of the drugs can cross the blood-brain barrier.

- Heroin and fentanyl are much more fat soluble and can reach the brain faster. They are much more potent when injected.

- Opioids easily cross the placenta. Newborns can suffer withdrawal symptoms but can be stabilized with low doses of opioids.

Opioids: Metabolism

- Morphine reaches peak levels with oral administration within 60 minutes; with IV injection, within 15 minutes. The drug has a half-life of about 90 minutes to 3 hours.

- Fentanyl: with IV injection, peaks in 1 minute; half-life of 1.5 hours.

- Oxycodone: oral administration peaks in 30-60 minutes (controlled release 3 hours); half-life is 3-5 hours.

- Oral administration: first-pass metabolism in the liver reduces the bio-availability of opioids.

- Most opioids are metabolized via CYP-mediated oxidation (codeine, oxycodone, methadone) and have substantial drug interaction potential (with the exception of morphine).

Opioids: Excretion

- After metabolism in the liver, most opioid metabolites are excreted in the urine within 24 hours.

- Typically, morphine can be detected in urine for 1-2 days. In cases of heavy or chronic use, morphine might be detectable for slightly longer, but it usually can’t be detected after about 4-5 days.

Pharmacodynamics: Effects of Opioids

- Effects of opioids on the CNS are related to dose and rate of absorption.

- Low to moderate doses result in:

pain relief (analgesia)

relaxation

dreamy sleep

- Some researchers suggest morphine relieves anxiety, aggression, and feelings of inadequacy. This may lead to more drug use.

- At higher doses, there is an abnormal state of elation or euphoria, described as a “kick,” “bang,” or “rush.” This acts as a powerful reinforcer that encourages repeated drug use.

Pharmacodynamics: Side Effects

(A) Behavioral

- drowsiness, inability to concentrate

- (rarely) adverse effects, such as dysphoria, restlessness and anxiety

- At highest doses, the sedative effects may lead to unconsciousness.

(B) Physiological

- constricted pupils

- nausea and vomiting. Opioids affect the area postrema in the brain stem that elicits vomiting.

- constipation: Opium and morphine have been used to treat diarrhea and can be life-saving to stop fluid loss in severe bacterial and parasitic diseases.

Opioid Overdose

- at highest doses = respiratory depression. In recreational users, tolerance to euphoria develops faster than to respiratory depression.

- Opioids act on the brain stem’s respiratory center; respiratory failure is the ultimate cause of death in overdose.

- sedative effects may lead to loss of consciousness.

- body temperature and blood pressure fall

- pupils become very constricted

- antidote = naloxone (Narcan)

Opioid agonists = morphine, oxycodone, fentanyl, etc.

Opioid antagonists = naloxone, naltrexone

Neurochemical Effects: Receptors and Endogenous Opioids

- Our bodies synthesize our own analgesic substances: endogenous opioids (endorphin, enkephalin, dynorphin)

- Endogenous = produced in our body

- discovered in 1974

- produced in response to pain, but also to exercise, laughter, etc.

- Both opioid drugs and endogenous opioids produce their effects via endogenous opioid receptors in the CNS.

Analgesia - medial thalamus, periaqueductal gray (PAG), median raphe, spinal cord

Positive reinforcement - nucleus accumbens, VTA

Cardiovascular and respiratory depression, cough control, nausea and vomiting - brainstem

Opioids: Mechanism of Action

- Opioid receptors are metabotropic.

- Opioids inhibit nerve activity in multiple ways:

Postsynaptic inhibition - receptors activate a G protein that opens K+ channels to hyperpolarize the post-synaptic cells, reducing firing rate.

Axoaxonic inhibition - receptors activate G proteins that close Ca2+ channels, reducing the release of neurotransmitter.

Pain Pathways to the Brain

- How do we feel pain?

- Painful stimuli can be detected by special receptors (nociceptors) located all over our body (including in our skin).

- Sensory information is sent through the spinal cord to the brain, where painful sensation is formed.

- Nociceptors --> Spinal cord --> Thalamus --> Cortex

Pain Management

- Multiple regions in the brain can suppress activity of the pain sensory neurons in the spinal cord.

- PAG (periaqueductal gray) is the key structure.

(I) Opioids stimulate neurons in the PAG that are responsible for inhibition of the pain sensory neurons in the spinal cord.

(II) Opioids directly inhibit the pain sensory neurons in the spinal cord.

(III) Opioids also affect higher sensory areas, hypothalamus and limbic structures in the brain.

Opioids: Reward Pathway

Reward pathway: mesolimbic: VTA ---> Nacc

- Opioids suppress GABA synapses on VTA dopaminergic neurons

--> Disinhibition --> Increase in firing --> Increase in dopamine release in Nacc

- Experiment: opioids micro-injected into the VTA increase dopaminergic cell firing

- Continued activation of the dopaminergic reward pathway leads to the feelings of euphoria and the ‘high’ associated with opiate use

Chronic Use of Opioids

- Chronic use of opioids leads to neuro-adaptive changes, which are responsible for tolerance, sensitization, and dependence.

- Opioids have significant reinforcing properties.

- Opioids effectively produce tolerance.

- Cross-tolerance among the opioids also exists.

- Example: after chronic heroin use, codeine will elicit a milder-than-normal response even if the individual has never used codeine before.

- Physical dependence: neuro-adaptive state in response to long-term occupation of opioid receptors.

- Physical dependence does not necessarily lead to abuse or addiction.

- When the drug is no longer present, cell function returns to normal and overshoots basal levels. Effects are seen in withdrawal symptoms (abstinence syndrome).

- Opioids in general depress CNS function; opioid withdrawal is rebound hyperactivity.

- Abstinence signs reflect a loss of inhibitory opioid action at all receptors in the CNS and elsewhere, as blood levels of the drug gradually decline.

- Severity and time course of withdrawal symptoms can vary with many factors, including the particular drug used:

Heroin: peak within few minutes; withdrawal may begin within 6-24 hours of discontinuation of the drug

Methadone: gradual increase over several days and a gradual decrease over several weeks

- Drug’s time frame can fluctuate with the degree of tolerance as well as the amount of the last consumed dose.

- Withdrawal symptoms can also be classically conditioned.

- The high rate of relapse may be due to the conditioned abstinence syndrome in the old environment.

- Some addicts describe withdrawal symptoms when they visit areas of prior drug use, even years later.

Opioid Addiction

DSM-5: Opioid Use Disorder

- A problematic pattern of opioid use leading to clinically significant impairment or distress, as manifested by at least two of the 11 criteria, occurring within a 12-month period.

Treatment

- A multidimensional approach includes detoxification, pharmacological support, and group or individual counseling.

- Counseling helps addicts identify the environmental cues that trigger relapse and design a behavioral response to those cues.

- Narcotics Anonymous is another option, based on the program for alcohol abuse.

Detoxification is the first step, which can be assisted by opioids such as methadone and buprenorphine (opioid receptor agonists):

substitutes for heroin

reduce symptoms to a comfortable level

Methadone maintenance program:

The most common and effective treatment for heroin addiction. Relieves craving for heroin.

Methadone is long-acting, producing a constant level of drug in the blood.

Methadone has cross-dependence with heroin, which prevents severe withdrawal symptoms.

Methadone can produce a “high” if injected, which could lead to illegal diversion of the drug.

Thus, programs require daily supervised oral administration. Little or no euphoria occurs with oral administration.

Oral administration reduces use of the needle by the addict and the ritual surrounding its use.

- Some treatment programs use narcotic antagonists (= opioid receptor antagonists).

Naltrexone (Trexan) is most commonly used because it has a longer duration of action than naloxone, is effective when taken orally, and has few side effects.

This method is effective for highly motivated individuals. Craving for the drug is not eliminated, so most less-motivated addicts stop antagonist treatment and return to drug use.

Experimental Treatment:

A vaccine is being developed to produce antibodies that would bind to the drug molecules in the blood circulation and prevent entry into the brain.

A vaccine that recognizes heroin and its active metabolites has been tested in rats.

#drugs and behavior #neuroscience #study blog #my notes

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spookysaladchaos · 19 days

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Global Top 5 Companies Accounted for 74% of total Buprenorphine Hydrochloride market (QYResearch, 2021)

Buprenorphine hydrochloride, a white crystalline powder, is a semisynthetic opioid analgesic used for the relief of moderate to severe pain. It is in the same chemical family of morphine, codeine and heroin. However, buprenorphine hydrochloride has the distinction of producing less euphoric effects than those drugs.

According to the new market research report “Global Buprenorphine Hydrochloride Market Report 2023-2029”, published by QYResearch, the global Buprenorphine Hydrochloride market size is projected to reach USD 0.16 billion by 2029, at a CAGR of 1.7% during the forecast period.

Figure. Global Buprenorphine Hydrochloride Market Size (US$ Million), 2018-2029

Figure. Global Buprenorphine Hydrochloride Top 12 Players Ranking and Market Share（Based on data of 2021, Continually updated）

The global key manufacturers of Buprenorphine Hydrochloride include Siegfried, Sanofi, Johnson Matthey, Mallinckrodt, Noramco, Faranshimi, Micro Orgo Chem, Unichemlabs, Arevipharma, Resonance-labs, etc. In 2020, the global top five players had a share approximately 74.0% in terms of revenue.

About QYResearch

QYResearch founded in California, USA in 2007.It is a leading global market research and consulting company. With over 16 years’ experience and professional research team in various cities over the world QY Research focuses on management consulting, database and seminar services, IPO consulting, industry chain research and customized research to help our clients in providing non-linear revenue model and make them successful. We are globally recognized for our expansive portfolio of services, good corporate citizenship, and our strong commitment to sustainability. Up to now, we have cooperated with more than 60,000 clients across five continents. Let’s work closely with you and build a bold and better future.

QYResearch is a world-renowned large-scale consulting company. The industry covers various high-tech industry chain market segments, spanning the semiconductor industry chain (semiconductor equipment and parts, semiconductor materials, ICs, Foundry, packaging and testing, discrete devices, sensors, optoelectronic devices), photovoltaic industry chain (equipment, cells, modules, auxiliary material brackets, inverters, power station terminals), new energy automobile industry chain (batteries and materials, auto parts, batteries, motors, electronic control, automotive semiconductors, etc.), communication industry chain (communication system equipment, terminal equipment, electronic components, RF front-end, optical modules, 4G/5G/6G, broadband, IoT, digital economy, AI), advanced materials industry Chain (metal materials, polymer materials, ceramic materials, nano materials, etc.), machinery manufacturing industry chain (CNC machine tools, construction machinery, electrical machinery, 3C automation, industrial robots, lasers, industrial control, drones), food, beverages and pharmaceuticals, medical equipment, agriculture, etc.

For more information, please contact the following e-mail address:

Email: [email protected]

Website: https://www.qyresearch.com

#Buprenorphine Hydrochloride

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oxycodone-medicine · 1 month

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Oxycodone

Oxycodone is utilized for the treatment of moderate to extreme agony in grown-ups. You could catch wind of it from a specialist in the event of serious torment medicines or on the other hand if the non-narcotic treatment isn't showing any improvement in the circumstance. Oxycodone is a narcotic medication that can prompt propensity development and misuse. It ought not be taken as an ordinary torment replacement medicine; it is for a few excellent cases in particular. It is a narcotic pain relieving that fundamentally impacts the manner in which the cerebrum answers torment. Oxycodone is additionally accessible in mix with acetaminophen, ibuprofen, and ibuprofen. Prior to utilizing such mixes make certain to peruse the fixings and take the medicine from a specialist or drug specialist.

The medication is a semisynthetic medication accessible in different delivery structures. As a prompt delivery item, treating moderate agony and now and then extreme sort of pain is basically utilized. Though in the lengthy delivery structure, it is utilized to get high serious degrees of ongoing agony that require a significant stretch of treatment.

Oxycodone 5 mg

A prescribed strong pain medicine Oxycodone 5mg is an opioid drug used to treat severe pain found in several products such as Percocet, oxytocin, and Endocet. The drug oxycodone 5 mg opinie provides long-term pain relief to the patient, so the patient doesn’t have to take another pill as often. It comes in different dosage forms including tablets, capsules, and oral liquid.

Oxycodone 10 mg

The 10 mg strength of oxycodone refers to the amount of the active ingredient in each tablet or capsule. This dose is typically prescribed when a higher strength is needed to manage more intense or chronic pain. However, the dosage should be carefully determined by a healthcare professional and adjusted based on the patient’s individual needs, medical condition, and tolerance.

Oxycodone 15 mg

A prescribed medicine brand name oxycodone 15 is used to relieve severe chronic pain. The product of Oxycodone works as an abused drug and is sold out under various brand names such as Roxicodone and Oxycontin. Sometimes overdosing leads to addiction which is very dangerous to health and causes many unwanted side effects like laziness, dizziness, dry mouth, and such.

Oxycodone 20 mg

This 20mg Oxycodone medicine helps in reducing moderate to severe pain. The Oxycodone 20 mg pills are analgesic medications. Oxycodone 20 mg follows up on the central nervous system (CNS) to relieve pain. It affects your brain to change how your body feels and reacts to pain.

This medicine is not meant for mild pain or when non-narcotic medication is effective. This medicine is not made for treating that pain, which you only have once in a while or “as needed”. 20 milligram Oxycodone may convert into addiction-forming. Taking this pill can cause physical dependence and addiction.

Oxycodone 30 mg

Oxycodone 30(blue pill 30 mg oxycodone), sold under different brand names like Roxicodone and OxyContin, is a semi-manufactured opiate utilized helpfully for the treatment of moderate to ludicrous torture. It is altogether inclination outlining and is a normally abused drug. It is regularly taken by mouth and is open in fast movement and controlled-discharge definitions.

Oxycodone 40 mg

Oxycodone 40 mg pills are used for treating pain in patients suffering from chronic issues such as surgery pain, pain during cancer treatment, etc. These pills are used in patients who require round-the-clock treatment and when other medications do not work properly. The 40 mg pills are round in shape, yellow-colored bi-convex tablets. It belongs to the family of opioid analgesics. These pills work by binding themselves to opioid receptors and thus change how the brain feels about pain.

Oxycodone 60 mg

Oxycodone 60 mg is an opioid that belongs to the painkiller family and is used to treat moderate to severe pain. It is an oral and prescription medicine and is available in round orange-colored pills. These are the FDA-approved pain relief medicines extracted from roots of thebaine.

Despite being in demand, these pills come with a wide variety of side effects if abused or overused. The side effects include Abdominal pain, Dizziness, fatigue, and as such. Hence it is advised to take pills only with the proper medical guidance.

Oxycodone 80 mg

Oxycodone 80 is an opioid painkiller medicine that is used to treat moderate to severe pain. It is an oral and prescription medicine. Oxy pills work by manipulating the brain cells into believing that the pain has reduced to significant levels. It is made with a semi-synthetic opioid that works by binding itself to an opioid receptor to activate it.

Oxy 80 mg pills are one of the most in-demand pain relief medicines on the market. But they do come with common to severe side effects and hence should not be taken without a doctor’s prescription.

Oxycodone is widely available in 5 mg, 10 mg, 15 mg, 20 mg, 30 mg, 40 mg, 60 mg, 80 mg.

#medicine #health #newlifemedix

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rustedskyprisms · 2 months

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No but it’s true these people sound so dumb when they go on about “natural” stuff being all that is safe and then they take LSD or MDMA or anything else that is semisynthetic/synthetic.

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rilifegujarat · 3 months

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https://www.rilife.co/infrastructure/

Amoxicillin Trihydrate

Amoxicillin trihydrate is verbal semisynthetic penicillin, which offers antibacterial movement against Gram-positive and a narrow pastureland of Gram-negative organisms. Its way of activity affects the inhibition of bacterial cell separator synthesis.

#AmoxicillinTrihydrate #Amoxicillin #Trihydrate

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shivame124 · 4 months

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Top Synthetic & Semi-synthetic Lubricants

Synthetic & Semisynthetic Lubricants products represent the pinnacle of advanced lubrication technology. When seeking the best in Synthetic & Semi-synthetic Lubricants, look for a trusted supplier who offers superior formulations that enhance machinery performance and longevity. These top-quality lubricants ensure smoother operations, reduced friction, and increased equipment life, making them an indispensable choice for various industrial and automotive applications.

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omkarpatel · 5 months

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Thebaine Market is Estimated to Witness High Growth Owing to Opportunity to Treat Pain Management

Thebaine is an important alkaloid extracted from opium poppies. It is being increasingly used for the production of prescription pain medications and other opioids such as oxycodone and hydrocodone owing to its analgesic properties. Thebaine blocks stimuli that usually cause pain and produces general effects on the central nervous system and body similar to morphine. It is an important intermediate in the production of a variety of opioid pharmaceuticals.

The global Thebaine Market is estimated to be valued at US$ 92 million in 2023 and is expected to exhibit a CAGR of 1.5% over the forecast period 2023. Market Opportunity: Opportunity to Treat Pain Management The pain management industry has been exhibiting strong growth globally. According to WHO, at least 1.5 billion people suffer from some form of chronic pain. The rising prevalence of diseases requiring long term pain management such as arthritis, cancer etc. as well as the growing aging population are contributing to this market growth.Thebaine has emerged as an important alkaloid for production of various semisynthetic opioids and pain medications owing to its analgesic properties.The growing demand for effective pain management drugs worldwide is expected to drive the opportunities for Thebaine market over the forecast period. Porter's Analysis Threat of new entrants: Low capital requirements and limited technology in manufacturing make the threat of new entrants moderate. However, established players have economies of scale and supply chain advantages. Bargaining power of buyers: Buyers have moderate bargaining power as there are a few big pharma companies that account for majority demand. Buyers can negotiate on price and quality standards. Bargaining power of suppliers: Suppliers of raw material like opium have high bargaining power due to limited supply sources and supplier concentration in certain regions. Suppliers can negotiate on price and supply contracts. Threat of new substitutes: There are limited substitutes for thebaine given its unique properties required in manufacturing semi-synthetic opioids. Potential substitutes require significant R&D investments. Competitive rivalry: The market has few big players with capacity to scale up production. Price competition and new product development leads to high rivalry. SWOT Analysis Strengths: Established supply chain and large production capacity for major players. Thebaine is a crucial API for pharmaceutical opioids. Weaknesses: Susceptibility to regulations on opium cultivation and production. Supply disruption risks due to geopolitical issues in major growing regions. Opportunities: Growing demand for pain management drugs globally drives market potential. Technological advances can reduce dependence on natural opium supply. Threats: Stringent regulations to curb non-medical use threaten market prospects. Public awareness campaigns reduce social acceptability of opioid drugs. Key Takeaways The global Thebaine market is expected to witness moderate growth over the forecast period supported by increasing chronic pain cases worldwide. North America dominated the market in 2022 owing to higher consumption of opioid drugs for pain management in the region. However, regulations aimed at opioid overuse may impact prospects. Europe is anticipated to be the fastest growing market for Thebaine between 2023-2030 backed by rising pharmaceutical manufacturing in countries like Germany and established R&D facilities. Key players operating in the Thebaine market are Mallinckrodt pharmaceuticals, Noramco, Alcaliber, Tasmanian Alkaloids, and Sun Pharmaceutical Industries. These players dominate production andAPI supply worldwide and are investing in dependent technologies and partnerships for sustainable growth.

#healthcare

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ainews · 5 months

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Simvastatin is becoming an increasingly popular drug for orchids. Specifically, the drug is being used as a means of treatment for fungal diseases in these beautiful and hardy flowers. The drug is highly effective when used in combination with other treatments and has been observed to increase orchid survival rates considerably.

Simvastatin is a semisynthetic drug, meaning that it is derived from an existing molecule in nature. By manipulating this existing molecule, researchers were able to create an extremely potent yet highly customized drug. The potency of the drug makes it the perfect solution for treating fungal infection in orchids.

Besides its potency, another benefit of using simvastatin for orchids is that the drug is very safe. Simvastatin is more water-soluble than many other anti-fungal treatments, which means that it is quickly and easily flushed out of the body. This reduces the risk of any unintended or harmful side effects to the orchid.

Finally, simvastatin has shown to be effective against a broad spectrum of fungi, including oomycetes. Thanks to its terpenoid core, the drug can bind to the cell wall of the targeted fungus, ensuring disruption of the fungal cell membrane and death of the fungi.

All in all, it is clear to see why simvastatin is becoming a more popular treatment option for fungal infection in orchids. Not only is the drug potent and safe to use, but it is also effective against a wide variety of fungi. For these reasons, simvastatin is certainly a drug worth considering when taking care of your orchid friends.

#ai generated #fake news

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loftlynch35 · 6 months

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