Abilify and caffeine

Luara A Batista et al. Naunyn Schmiedebergs Arch Pharmacol. 2016 Jan.

. 2016 Jan;389(1):11-6.

doi: 10.1007/s00210-015-1170-x. Epub 2015 Aug 29.

Authors

Luara A Batista  ¹ , Thércia G Viana  ² , Vívian T Silveira  ² , Daniele C Aguiar  ² , Fabrício A Moreira  ³

Affiliations

• ¹ Graduate School in Neuroscience, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Belo Horizonte, Brazil.
• ² Department of Pharmacology, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Av. Pres. Antônio Carlos 6627, Belo Horizonte, MG, 31270-901, Brazil.
• ³ Department of Pharmacology, Institute of Biological Sciences, Universidade Federal de Minas Gerais, Av. Pres. Antônio Carlos 6627, Belo Horizonte, MG, 31270-901, Brazil. [email protected].

• PMID: 26319049
• DOI: 10.1007/s00210-015-1170-x

Abstract

Aripiprazole is an antipsychotic that acts as a partial agonist at dopamine D2 receptors. In addition to its antipsychotic activity, this compound blocks the effects of some psychostimulant drugs. It has not been verified, however, if aripiprazole interferes with the effects of caffeine. Hence, this study tested the hypothesis that aripiprazole prevents caffeine-induced hyperlocomotion and investigated the effects of these drugs on neural activity in the striatum. Male Swiss mice received injections of vehicle or antipsychotic drugs followed by vehicle or caffeine. Locomotion was analyzed in a circular arena and c-Fos protein expression was quantified in the dorsolateral, dorsomedial, and ventrolateral striatum, and in the core and shell regions of nucleus accumbens. Aripiprazole (0.1, 1, and 10 mg/kg) prevented caffeine (10 mg/kg)-induced hyperlocomotion at doses that do not change basal locomotion. Haloperidol (0.01, 0.03, and 0.1 mg/kg) also decreased caffeine-induced hyperlocomotion at all doses, although at the two higher doses, this compound reduced basal locomotion. Immunohistochemistry analysis showed that aripiprazole increases c-Fos protein expression in all regions studied, whereas caffeine did not alter c-Fos protein expression. Combined treatment of aripiprazole and caffeine resulted in a decrease in the number of c-Fos positive cells as compared to the group receiving aripiprazole alone. In conclusion, aripiprazole prevents caffeine-induced hyperlocomotion and increases neural activation in the striatum. This latter effect is reduced by subsequent administration of caffeine. These results advance our understanding on the pharmacological profile of aripiprazole.

Keywords: Antipsychotic; Aripiprazole; Caffeine; Striatum.

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Photo exhibition "Psychiatry kills" + Ode to Abilify: a_n_j — LiveJournal

Exhibition stands

Organizer - CCHR - Civil Commission on Human Rights.

The Citizens Commission on Human Rights (CCHR) was founded in 1969 to investigate and publicize violations of human rights in psychiatry and to bring order to the treatment of mental illness.

I'll add from myself. I came to this conclusion, specific, about a specific (new) drug. Everyone has probably heard about it, since there is little that has ever had such aggressive advertising.
This is Abilify (ABILIFY, ABILIFAY, aripiprazole) - a new atypical antipsychotic, neuroleptic. This drug is prescribed for patients with almost all known mental illnesses and even for the treatment of alcoholism. That is, in fact, it is a panacea (I wonder if hemorrhoids are treated with it?). It is also used to treat depression. What do people in deep depression want? That's right - they don't want anything - they want to die. That is, depression, one might say, is equal to suicide. And it would be very logical to assume that drugs prescribed for depression should reduce this desire to die, or at least not increase it. But ... We are reading the "instructions for use" of this newest "panacea". No, no, we read what is written in VERY SMALL FONT (you may need a magnifying glass for this, or you can read through a bottle of water if depression does not allow you to get up from your chair to go to the store for a magnifying glass). We read: "Possible suicidal tendencies while taking and especially after stopping the drug." Are you truncating? Not yet?
How much does maintenance, treatment, etc. cost? patients in hospitals? How much does it cost to maintain the same patients after "treatment", say, shock therapy or after a lobotomy? Even though they are already in a plant state, these people want to eat, but they themselves are no longer able to earn money for food - more than half of the homeless on the streets of any city in any country are graduates of such "health centers". We have to help them exist in the state. level - disability pensions, etc. It's millions, billions of dollars. There is no profit from such "plants", only losses, and even at gas stations they stick with foam at the mouth. Exit? Gas chambers - purge of the nation and humanity. But this is inhumane, in our age, when defenders of human rights are ready to bite a person to death for his own rights! No, we are against fascism! Exit?
EUREKA! "PANACEA"! ABILIFE! You held on for 5-10-15-20... years on antidepressants, not feeling any improvement, still constantly seeing an open window out of the corner of your eye? But something at the very last moment stopped you, already standing on the windowsill and already "tasting the wind of liberation from the "treatment"? , which will help relieve the economy of the most humane in the world and democratic (and not only it)!0009 Abilify! - no more dirty, tattered and reduced to a vegetable state in hospitals with drugs and electric shock demi-humans at our bus stops and gas stations!

Abilify...

And, to be honest, I’m not so interested anymore whether it was just such a “side” suicidal effect of the “medicine” designed to fight it, or whether they thought about it for a long time, conducting experiments on cockroaches, mice, monkeys, and then on "the highest primates", the brightest heads of modern psychopharmacology? And from what tops, not from the very top, the Fuhrers, did they receive the task to "finally clear the world of sick (and often just deeply thinking) people"? In general, it does not matter, and we will never know for sure . ..

But will we continue to turn away from advertising - "Abilify! And the problems are gone!" - knowing that "as it never happened" - means "no person - no problem", means jumping out the window, under the train, off the cliff? . Moreover, it is often prescribed forcibly: either you drink a "panacea", or you are tied up in a hospital, and an electric current is connected to your temples.

I don't hide it under the cut, though it's a long text. Maybe someone will accidentally see and think...

PS. By the way, the headquarters of the Citizens' Commission on Human Rights is located not just anywhere, but... in Los Angeles. Another irony of my fate... :)

ZY2. I see a lot of young people trying to get advice on "cure" for depression, suicidal thoughts, etc. Almost everyone requires a panacea=drug. About medicines (this is not only Abilify - a "panacea". Each new "medicine" is announced by her ... before the "invention" of a new one, because after some time even the "plants" understand that they, as always, have been cheated again . ..) - read above and follow the links at the beginning of the post.

From the text of the photo exhibition linked above:
"In a book on clinical research on the impact of proper nutrition on the human state of mind, Melvin R. Werbach, MD, assistant professor at the University of California at Los Angeles (Medical Department), writes that the lack folic acid, vitamin B12, vitamin C and niacin is the source of what we call "depression."

From myself again: drink ascorbic acid, vitamin complexes (by the way, I didn’t like Red Bull in vain, even though I don’t have such a depression, and yet you shouldn’t drink a lot of it - I already felt it - it throws me into mania. Still - so much caffeine, but it contains a lot of vitamin B12), eat right (with fresh fruits and vegetables), healthy, on time, keep a sleep schedule, be in the bright sun more often, take sunbaths if possible (sunbathe, etc.) , be more often in the fresh air (by the sea, in the forests), water procedures (hot baths, contrast showers) are very helpful. In a word, no matter how trite it may sound - lead a healthy lifestyle, not locking yourself in the closets of the apartment and "pitying yourself, the unfortunate." Banal, yes. VERY trite. Well, or go on the unbeaten, non-banal pseudo-scientific paths with abilify and others like them. Only my "scientific" path almost stopped at the cliff in Malibu (by the way, it's a very beautiful place - I didn't choose it in vain :)
But I'm still here and I'm still hitting the keys while typing this post :)

and ZY3. (the last one :) It was the CCHR articles that helped me a lot in my time. I even printed one of the brochures in color - I always lay there. The Internet, of course, is "evil", but sometimes good too :) Now there are even more links, and more interesting in some ways, and even world traveling photo exhibitions, here, are held by people. Happy enlightenment :)

Funds that act primarily on the central nervous system

GBOU VPO First Moscow State Medical University. THEM. Sechenov Ministry of Health of the Russian Federation
Pharmaceutical Faculty
Department of Pharmacology
Funds operating
mainly at the central nervous system
Lecture 1,
Kudryashov Nikita Viktorovich
Pharmacology Department
Pharmaceutical Faculty
Moscow, 2015
funds
Normotimics (anti-manic)
Anxiolytics (tranquilizers)
Sedatives (sedatives)
Psychostimulants
Nootropics
NEUROLEPTICS (ANTIPSYCHOTIC DRUGS)
Antipsychotics include drugs intended for the treatment of
psychosis and other severe mental disorders.
Neuroleptics
(antipsychotics)
Typical
• More
block dopamine
receptors than serotonin

• Cause
drug
parkinsonism
Atypical
more block 900

9 Serotonin

0 mg (20009 /day)
Akathisia
Malignant
neuroleptic
syndrome
Dyskinesia
Hyperprolactinemia
Progressive rigidity,
hyperthermia, tremor, opisthotonus,
anxiety, confusion, etc.
Any violent
involuntary movements that
persist after discontinuation of the drug
Gynecomastia, impotence, menstrual irregularities

1) Immediate withdrawal
of the drug
2) Dantrolene (muscle relaxant)
3) Bromocriptine
1) After drug withdrawal
1) After drug withdrawal
reversible
Drug change
NB! More characteristic of typical antipsychotics
SIDE EFFECTS OF NEUROLEPTICS
2. Associated with other receptors
• Histamine receptors (H1): pronounced sedation and weight gain
• Muscarinic receptors: atropine-like action
• Alpha-adrenergic receptors: orthostatic hypobolism 3.9009 effects
• Hyperlipidemia and hyperglycemia (clozapine, olanzapine)
4. Cardiac effects
• Ventricular arrhythmia and sudden cardiac death (mostly
typical of older antipsychotics, such as thioridazine)
5. Other side effects
• Agranulocytosis (typical of clozapine)
• Dose-dependent seizures (typical of clozapine)
PEDIATRIC USE OF NEUROLEPTICS
• Antipsychotics are used to treat the manic phase of autism, bipolar 909090 disorders in children; and
schizophrenia in adolescents. Examples of antipsychotics used in children and
adolescents: aripiprazole (Abilify), risperidone
(rispolept).
• Haloperidol may be used to treat obsessive-compulsive disorder in children and adolescents, as
antidepressant medications prescribed by adults to treat this condition may cause
adolescents to develop suicidal thoughts and behavior.
• Young patients are more sensitive to the side effects of
antipsychotics, in particular to the development of extrapyramidal disorders
and weight gain, so treatment should be carried out with
the lowest effective dose.
• It should be remembered that risperidone can increase the level of
prolactin in the blood, which can lead to a delay in
puberty. As a rule, tolerance develops gradually (in
within 12 months) to hyperprolactinemia.
NORMOTHYMICAL DRUGS
A group of drugs capable of stabilizing mood in mentally
patients, primarily those suffering from bipolar affective disorder
(previously called manic-depressive psychosis)
1. Lithium salts
• Lithium carbonate
• Lithium citrate
2. Anticonvulsants
• Valproic acid
• Carbamazepine
• Lamotrigine
signal
The mechanism of action of lithium salts is not exactly
established,
it is believed that
the
therapeutic effect of lithium is associated with the effect on brain monoamines
of the brain, namely with a change
in the transmission of dopamine - a decrease
of its release from the synapse and a violation of
signal transmission from dopamine receptors
through the inositol phosphate system
.
LITHIUM SALTS
Uses: bipolar affective disorder, resistant forms of depression

Side effects:
• Tremor, avoid caffeinated drinks,
reduce lithium dose, it is also possible to eliminate tremor with propranolol
(at a starting dose of 20 mg / day and target 160 mg/day)
• Polyuria and compensatory polydipsia (blood
control of urea and nitrogen)
• Hypothyroidism (requires control of thyroid function)
• Sinus bradycardia and AV block possible with overdose
• Use in early pregnancy may lead to
development of cardiac abnormalities in fetus
• Sustained increase in polymorphonuclear leukocytes with long-term use

• Metallic taste in the mouth
ANXIOLYTICS (TRANQUILIZERS)
Anxiolytics are drugs that reduce feeling
anxiety and fear
Anxiolytics
drugs,
Anxiolytics of the benzodiazepine series
the difference is that
• Diazepam (Relanium)
benzodiazepines are not suitable for
• Phenazepam
long-term therapy for more than
• Clonazepam 1-92009 are greater
• Alprazolam (Xanax)
degree
drugs
for
Non-benzodiazepine anxiolytics
relief
anxiety
• Buspirone
symptomatic
• Afobazole
• Hydoxizine (Atarax)
Antidepressants
• The listed
Preparations
Actually
• Flovkamin (Fevarin)
Anxiolytics are not, however,
• Paroxetine (Paxil)
Successfully
for a long -term
• Citalopram (citramil)
therapies
therapies are used anxiety disorders such as
• Escitalopram (cipralex)
generalized anxiety disorder,
• Venlafaxine (velaxin)
panic attacks, social phobia, agoraphobia,
obsessive-compulsive disorder, etc.
• Amitriptyline
• Beta-blockers can be used for fear
• Clomipramine (anafranil)
public speaking and for elimination
Beta-blockers
tachycardia for panic attacks
KHANAPRIM0MEI
Benzodiazepines Target: benzodiazepine binding site on the GABA
receptor 1. Benzodiazepines bind to the
benzodiazepine site on the
GABA receptor
2. Conformation of the entire GABAA receptor
3. The affinity of the GABAA receptor for GABA
increases 4. Chlorine channels
formed by the GABAA
receptor open
5. The supply of
chlorine to CNS neurons increases
6. The process of hyperpolarization of
membranes
GAMAA-
CNS neurons develops GABA
Benzodiazepines
NB! The mechanism of action of benzodiazepines is carried out according to the principle of
allosteric regulation of the GABA receptor
PHARMACOLOGICAL EFFECTS OF BENZODIAZEPINES
1.
2.
3.
4.
5.
6.
Dominatory effect
Sedative effect
Anxiolytic effect
Pis -rod effect
Anti -icing effect
amnestic effect (anterograd amnesia)
Side effects of benzodiazepines:
• Dreamy, vice versa, vice , decreased concentration and attention
• Decreased libido and erectile dysfunction
• Depression and disinhibition
• Hypotension and respiratory depression (with intravenous administration, or with
pathologies of the respiratory and cardiovascular systems)
• Withdrawal syndrome
• Risk of drug dependence
• Anterograde amnesia
NB! In case of benzodiazepine poisoning, the drug flumazenil is used,
which is an antidote for benzodiazepines
BUSPIRON
Buspirone is an anxiolytic with a serotonergic mechanism of action,
the drug is a partial agonist of serotonin 5-HT1A receptors. In addition, buspirone can block a number of dopamine
receptors.
Indications for use:
• Anxiety disorders
Side effects:
• Dizziness, headache
• Drowsiness
• Premature ejaculation
NB! Compared to anxiolytics of the benzodiazepine series
, the anxiolytic effect develops later and there is no
narcotic potential.
Under 18 is contraindicated!
AFOBAZOL
The drug is an agonist of sigma-1 receptors and through their activation
positively modulates the GABA-receptor, increasing the affinity of GABA to
GABAA receptor. In addition, afobazole has activity against
melatonin receptors and the MAO-A enzyme. It also has an antidepressant effect

Indications for use:
• Anxiety disorders
• Nicotine addiction (smoking cessation)
Side effects:
• Allergic reactions
• Nausea
• Headache
Features of the drug:
• Anxiolytic effect develops on 3- Day 7 of taking
• Less effective for panic attacks than other anxiety attacks
disorders
• When taking the drug, drug dependence and addiction do not develop

• Contraindicated under 18 years of age.
SEDATIVES
Medicines that have a general sedative effect on the CNS.
The sedative (calming) effect is manifested in a decrease in the reaction of
to various external stimuli and a slight decrease in daytime
activity.
Preparations containing bromine
• Bromkafmora
Herbal preparations
• Valerian root rhizomes (extracts, tincture)
or combined herbal preparations -
Persen, Persen forte, Persen nocturnal
Valerian-based sedatives have a complex mechanism of
sedative action:
• Stimulate benzodiazepine receptors
• Disrupt neuronal reuptake
• Interact with adenosine receptors
A number of different pharmacological agents also have a sedative effect
: benzodiazepines, barbiturates, antipsychotics,
antihistamines, some antidepressants.
PSYCHOSTIMULATORS
Substances capable of enhancing the mental and, to a lesser extent, physical activity of the
organism of both healthy and sick persons.
Xanthine derivatives
• Caffeine
Phenylalkylamine derivatives
• Amphetamine
Sydnonimine derivatives
• Mesocarb (sidnocarb)
Currently not used in
medical practice on the territory of the Russian Federation!
Scope of psychostimulants:
• Asthenic
conditions
and
neurotic
disorders,
accompanied by retardation, lethargy, apathy, decreased performance

• Correction of side effects of neuroleptics and tranquilizers
of the benzodiazepine series
• Mental retardation and other development in children, etc.
• In the US and EU countries, psychostimulants, including
amphetamine derivatives, are used in pediatric practice for the treatment of
attention deficit hyperactivity disorder (one of the main
drugs - methylphenidate under auction. The name "Ritalin"), however,
Along with psychostimulants are used by other drugs: clonidine,
Guanfacin and atomoxetine (Stratter)
Psychostimulants
Dopamineps
Noraaps


Biosynthesis
Biosynthesis
DAS
DASSITIONS. MAO-B
Metabolites
MAO-B
Mesocarb
DAT
MAO-A
NA
NAT
YES
Amphetamine
HA
Dopamine receptor


80% of mediator
is reuptaken into
synapse!
Adrenergic receptor
Effect
Reductions:
Yes - Dopamine
MAO - Monoaminoxidase
DATA - Dopamine conveyor
NAT - Norepinephrine
On - Norepinephone
Effect
Mesocarb (Synocarb)
Mechanism of action:
is much more violated
than dopamine in the CNS. The psychostimulating effect is due mainly to
way, the accumulation of norepinephrine in the synaptic cleft.
Indications for use:
• Asthenic
conditions
and
neurotic disorders
, accompanied by
lethargy, lethargy, apathy, decreased working capacity
, etc.
• In children: mental retardation, weakness, organic
diseases of the central nervous system with a predominance of lethargy, lethargy, asthenia.
Side effects:
• Headache
• Irritability
• Insomnia
• Decreased appetite
• Increased blood pressure
• Exacerbations are possible in patients with positive symptoms of psychosis
NB! Side effects, as well as the main effect, are mainly
due to an increased content of NA in the CNS
CAFFEINE
Mechanism of action:
• Caffeine inhibits the enzyme phosphodiesterase, thereby increasing the content of cAMP in target cells

• Blocks adenosine receptors of subtype 1
• Inhibits acetylcholinesterase
• Increases the mobilization of calcium ions from the intracellular depot
• Stimulates the respiratory and vasomotor centers
Pharmacological effects:
• Psychostimulatory effect
• Analeptic effect
• Increased blood pressure (with hypotension), cardiovascular system and heart rate (cardiotonic)
• Diuretic effect
Application:
• Diseases and conditions accompanied by depression of functions CNS,
CCC and respiratory system, incl. drug poisoning

• Spasms of cerebral vessels
• Decreased mental and physical performance
• Breathing disorders in newborns
Side effects:
• Anxiety, insomnia, tachycardia, arrhythmias, increased blood pressure, nausea, vomiting,
tremor
NOOTROPIC DRUGS
Neurometabolic stimulants with a specific effect
on the central nervous system, improving learning and memory
Piracetam (nootropil) facilitates learning processes and improves memory.
Like psychostimulants, the drug increases mental performance
, but does not have side effects inherent in psychostimulants
effects.
• The processes of memory and learning are the highest forms of
adaptation.
• Memory and learning decline with age, as a result of
neurogenic stress, intoxication, neurodegenerative diseases,
brain injury, stroke, and so on.
How do nootropics work?
Memory and
learning
Nootropics
N-cholinores
NMDA-R
AMPA-R
5-HT-R
The scheme is taken from the lecture "Receptors in pharmacology: practical application", Kovalev G. I., MD ., prof., head. laboratory
radioisotope research methods FSBSI Research Institute of Pharmacology named after V.V. Zakusova.
Classification of drugs with nootropic effect
1. Directly nootropic effects
A. Derivatives Pyrrolidone
• Piracetam (nootropil)
B. Gamkergic preparations
• GABA (Aminalon) C. Glutamatergic drugs
• Glycine
2. Indirect nootropic drugs
A. Antioxidants and membrane protectors
• Mexidol
B. Neuropeptides and their analogs
• Semax
C. Calcium channel blockers
• Cinnarizine
• Nimodipine
D. Cerebral vasodilators
• Vinpocetine (Cavinton)
• Nimodipine (Nitop) • G00dingo E90 Herbal remedies
biloba (tanakan, bilobil, etc.)
Based on the materials of the lecture “Receptors in pharmacology: practical application”, G.I. Kovalev, MD, prof., head. laboratory
of radioisotope research methods of the V.V. Zakusova.
FEATURES OF NOOTROPIC DRUGS
Effect on the pathology of mnestic functions
Accumulative nature of action
Systemic reaction to the drug
Diversity in the mechanism of action
Diversity in chemical structure MD, prof. , head. laboratory
of radioisotope research methods of the V.V. Zakusova.

29. Potential targets for nootropics

• 
  Types of abandonment issues
• 
  Third wave cbt therapies
• 
  How not to be petty
• 
  Loving after divorce
• 
  How to get involved in local community
• 
  Funny babies cartoon
• 
  How to cope with aging parents
• 
  Major depressive diagnosis
• 
  Estranged mothers and daughters
• 
  Definition of narcissistic abuse
• 
  Anxiety while trying to fall asleep