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Anticoagulants and Pharmacokinetic Principles

Fentanyl

Fentanyl is mainly respired; once ingested, it is absorbed into the bloodstream, and the most primitive and sensitive part of the brain is sensitized. As a result, dopamine levels in the brain are increased, which gives a rewarding experience (Vice, 2016). The dopamine surge in the brain and its effects of increasing your activity levels make one always desire to use the drug often. The pharmacokinetic principle that best associated with the physical withdrawal symptoms is the distribution to the body. Fentanyl is mainly distributed to the brain, where it causes the increased release of dopamine. Once the pill is taken, one feels relaxed, functional, and energetic to carry out the day’s activities.

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Naloxone

The mechanism of action of naloxone is that it reverses the effects of opioids once they are overdosed and causes respiratory distress. Naloxone belongs to the chemical class of opiate antagonists. The anatomical part of the brain turned off during an overdose is the medulla oblongata. The dosage of naloxone administered for the reversal of an overdose is not adequate for reversing the side effects of an opioid (Vice, 2016). Naloxone has a short half-life, and the duration of action of the drug is usually short-term compared to opioids. For an individual to reverse the effects of the drugs, it is recommended that more than one dose of the drug be administered to the person. The use of naloxone, though, is likely to cause withdrawal symptoms as it reverses the effects of the opioids that are administered.

Suboxone

Suboxone is a mixture of medications, and it contains buprenorphine and naloxone. Once it is ingested into the body, it binds tightly to the dopamine receptors that the opioids bind to in the brain; this reduces the binding of the opioids. (Vice, 2016). When it binds to these receptors, it reduces the effects of opioids by reducing the intoxication of these drugs to the user. It also reduces the desires and cravings they have to use the opioids, and to some extent, allows the addicts to avoid abusing the opioids and return to a drug-free state.

The preferred route for Suboxone administration is sublingual, and the drug is allowed to dissolve through this route to increase its efficiency. Overdosing Suboxone is not as easy as it may seem as it is impossible for one to overdose on Suboxone singly (Vice, 2016). Suboxone is a drug that binds partially to the opiate receptors and specifically dopamine; hence, it does not produce high effects brought about by opioids. Thus, the drug limits the number of effects brought about by opioids and rarely brought about the side effects like slow breathing rates. An overdose of the drug may only occur when the drug is administered alongside drugs that slow down breathing rates, such as sedatives.

Heparin

Heparin is an anticoagulant drug that is administered subcutaneously and acts by activating antithrombin. Antithrombin is an anticoagulation factor, and it also accelerates the rate at which antithrombin inhibits the clotting enzymes. Heparin is administered once daily, and the dosage administered is usually 1 gram (Thrombosis, 2021). Therefore, it is mainly administered before surgery, and at this point, warfarin administration is usually stopped as its anticoagulant effect is usually outside the desired therapeutic range.

Warfarin

Warfarin, on the other hand, is an anticoagulant that is administered orally. Warfarin acts by inhibiting the y-carboxylation step by inactivating the enzyme epoxide reductase, thus reducing the release of the vitamin K-dependent factors for clotting, inhibiting clotting of blood (Thrombosis, 2021). Therefore, when transitioning heparin to warfarin, heparin is given alongside warfarin for a minimum of 4 to 6 days until blood is sufficiently thinned. Afterward, heparin therapy is withdrawn, and warfarin is given alone. The rationale for stopping heparin therapy is that continued administration may lead to heparin-induced thrombocytopenia.

Mechanism of Action Indicated Use Monitoring
(Test & Frequency)
Adverse Effects Drug Interactions
Apixaban (Eliquis®)
It prevents stroke and systemic embolisms.
Treatment of thromboembolic diseases and prevention of recurrence
Monitoring is not indicated as patients using this drug usually have standard prothrombin time and activated partial prothrombin time.
Frequent assessment is needed, however, for compliance and the need for changing the treatment.
Bleeding is a significant adverse effect that is associated with the administration of apixaban. Apixaban administration with drugs that induce or inhibit cytochrome3A4 and p-glycoprotein should be avoided as these patients are at an increased risk of bleeding. Such drugs may include and. are not limited to the azoles, macrolides, and antiretroviral protease inhibitors.
Dabigatran (Pradaxa®)
The treatment of thromboembolic diseases and prevention of the recurrence of these diseases
Prevent formation of systemic embolisms and also stroke
Activated partial prothrombin time is done to test dabigatran’s availability and is invariably prolonged in its presence.
Thrombin clotting time also is used to determine the effectiveness of dabigatran.
The significant adverse effect is bleeding
Another effect of dabigatran is dyspepsia.
The absorption of dabigatran is reduced by the agents that, when taken, increase the gastric pH, and this may include mainly the antacids reducing the efficacy of dabigatran.
Warfarin (Coumadin)
Treatment of acute venous thromboembolism
Long term prevention of venous thromboembolism
Prevention of stroke and the formation of embolisms in the various body systems
Frequent laboratory monitoring of patients is necessary, and they include:
First, the international normalizing ratio is done until it is stable, and then the patient is monitored every month after that.
Significant adverse effects are bleeding due to the inhibition of the clotting factors.
Other effects may include hair and skin loss.
It should not be administered by other drugs metabolized by the cytochrome p450.
Also, administration with other anticoagulation drugs increased the risks of bleeding.

References

Vice. (2016). Fentanyl: The Drug deadlier than heroin. Web.

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Thrombosis Canada. (2021). Clinical guides. Web.

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