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Beta blockers

Category: Medicines

Type

Involuntary

Introduction and description

Beta or ‘beta-adrenergic blocking agents’ are a class of drugs 'used for the management of cardiac arrhythmias, cardioprotection after myocardial infarction (heart attack), and hypertension'.

Quite a number of the drugs in this category have a history of providing involuntary spiritual experience in the form of hallucinations, out of body experiences and near death experiences. 

The drugs

There are five main adrenoceptors receptors.

The Beta 1 receptors are, in theory,  heart related.  The binding of an agonist to the beta–1 receptors generally causes a sympathetic response  -  the fight-or-flight response! The  heart rate will increase,  the pupils will dilate so we can see better to run, energy will be mobilised, and blood flow diverted from other non-essential organs to skeletal muscle. Go on a theme park ride and you will know exactly which receptors and agonists get going here!

But the antagonists stop all this happening, so the antagonist products tend to dilute the fight or flight response – the heart rate will decrease, the pupils will narrow, and energy may decrease and you may feel sedated.  There may also be considerable vasoconstriction leading to hypertension. Note this.

Beta blockers are all  beta adrenergic receptor antagonists, and reduce the effects of the endogenous epinephrine (adrenaline) and other stress hormones.   Beta blockers block the action of both epinephrine (adrenaline) and norepinephrine (noradrenaline) in particular, on adrenergic receptors, part of the sympathetic nervous system which mediates the "fight or flight" response. 

This is the theory.

 

Beta blockers are symptom based medicine.  They show naive thinking on the part of those who produce them, as the particular receptors they target can have knock-on effects in other areas, which in turn have an effect somewhere else.  As we can see they can produce hypertension and restrict the blood to the extremities of the body, for example.  The prescribing of them also ignores one rather fundamental fact.

Whatever caused the heart attack, or whatever is causing the arrhythmia or whatever caused the hypertension is still there in the body.  Arrhythmia, for example, can be caused by mineral imbalance.  Heart attacks can be caused by bacteria, toxins, fungi, viruses, parasites, radiation, heavy metals and other pharmaceuticals. 

If the cause is still present, it will carry on doing the damage, whatever symptom based medicine we use to counteract its effects.  This is why people taking these drugs get such apparently peculiar side effects.

 

For example, a quite common [apparent] side effect is hypertension and chest pain, which one would have thought the drugs in this class help not cause.  Look at the side-effects for Toprol xl.   Pneumonia, hypersensitivity, massive weight gain, malignant hypertension, convulsions, renal failure, myalgia.  What is the link?

People who take these drugs in the rather naive belief that they will help to 'cure' them, are bewildered that they should then get all the symptoms they had before the heart attack, only worse.  But of course they will be worse, if the cause has not been addressed.

Side effects

 The majority of the drugs on the market are not actually 'pure' beta 1 antagonists, many affect other receptors and one of the receptors which is affected is the beta 2 receptor.  This has its own set of problems, but the artificial invocation of the parasympathetic nervous system can be, on its own, very problematic:

Headaches result from the lack of oxygen

Dyspnea - One serious side-effect is shortness of breath, asthmatic like feelings and severe trouble breathing.  There is also a cough, which tends to be a reaction to this lack of air in the lungs - respiratory depression, but tightness in the chest.  Dyspnea is defined as 'shortness of breath (SOB), or air hunger,and is the subjective symptom of breathlessness.'  It isn't just subjective either, it is real and the lack of oxygen at night can cause appalling headaches.

Nightmares

Adverse effects of beta-adrenergic receptor blocking drugs can be divided into two categories:
1) those that result from known pharmacological consequences of beta-adrenergic receptor blockade; and
2) other reactions that do not appear to result from beta-adrenergic receptor blockade.
Adverse effects of the first type include:
 - bronchospasm,
 - heart failure,
 - prolonged hypoglycemia,
 - bradycardia,
 - heart block,
 - intermittent claudication, and
 - Raynaud's phenomenon.
Neurological reactions include depression, fatigue, and nightmares. .... Patient age does not appear, in itself, to be associated with more beta-blocker side effects. Side effects of the second category are rare. They include an unusual oculomucocutaneous reaction and the possibility of oncogenesis. There are also many drugs that interact with beta-blockers, which may increase toxicity.  PMID: 2895072

Raynaud's phenomenon

Raynaud's phenomenon or Raynaud phenomenon is excessively reduced blood flow to various parts of the body - usually the extremities - causing discoloration of the fingers, toes, and occasionally other areas. This condition may also cause nails to become brittle with longitudinal ridges.  Beta blockers, because they cause overall vasoconstriction to the extremities, can result in reduced blood flow to the hands and feet, causing these symptoms.

 Bradycardia - is a slow heart beat and is defined as a  resting heart rate of under 60 beats per minute, although it is seldom symptomatic until the rate drops below 50 BPM. Beta blockers aim to put less strain on the heart, but the problem is that bradycardia can result in fatigue, weakness, dizziness, and at very low rates fainting. A waking heart rate below 40 BPM is considered 'absolute bradycardia'.  At these low rates you can also get hallucinations and out of body experiences.  At extremely low values you are into near death territory.

Claudication, - that is impairment in walking, or pain, discomfort or tiredness in the legs that occurs during walking. Claudication is most common in the calves but it can also affect the feet, thighs, hips, buttocks, or arms. The word "claudication" comes from the Latin "claudicare" meaning to limp.  The cause is again the vasoconstriction of the arteries leading to the peripheral muscles.  Occasionally the cause may be the cause of all the problems in the first place - toxins, heavy metals, a virus or bacteria.  If you start getting gangrene you know it was bacteria.

Anaphylactic shock - one very alarming new finding is that beta blockers can send you into anaphylactic shock

Our anaphylaxis database indicated a higher risk of severe anaphylaxis after monotherapy with β-blockers or ACE inhibitors, which was more pronounced when both drugs were combined. This was confirmed in our mouse model. While single therapeutics had either no significant (ramipril) or a modestly aggravating (metoprolol) effect, their combined administration exacerbated anaphylactic symptoms potently and simultaneously enhanced MC mediators, hinting at MCs as direct targets PMID:  25441633

Erectile dysfunction -  beta blockers may contribute to erectile dysfunction.  An erection requires a heightened flow of blood to the penis, restrict that flow and you haven't got a hope in Hades of even raising a pennant.

 

Nowadays, erectile dysfunction (ED) is considered an increasingly important clinical condition in men with heart failure (HF) which may influence the therapeutic approach to these patients. Since there is cogent evidence that ED is a "sentinel marker" of acute cardiovascular events especially in men younger than 65 years or in those affected by type 2 diabetes mellitus, it deserves an early diagnosis and an appropriate treatment. ….. Moreover, it is well known that some classes of drugs, normally employed in the treatment of HF patients (e.g.thiazide diuretics, spironolactone and β-blockers), might worsen or even contribute to ED development. PMID:  23369145

And here we have a case report

from eHealthme case study report August 2014
Initially was given Metoprolol 25-50mg/day for high blood pressure 180/115. Was good and relaxed for about a week, then severe palpitations started to occur. Was taken off Metoprolol and put on Losartan 25-50mg/day and palpitations continued to be severe and frequent 2-5/day lasting a few minutes to an hour or two. Recovery was longer. Shortness of breath was accompanied. Was at cardiologist's office when a severe palpalitory event was occuring. He said I was having PAC's. I've been told PVC's as well in past visits to the doctors office. I stopped taking Losartan a week and a half ago. I've had several good days without palpitations occuring with a few days with severe palpitations occuring. I'm not sure if palpitations will cease, but I wasn't having palpitations or arrythmias prior to taking any of these medications. Again, I am seeing a marked improvement overall after ceasing these medications. I've lost 20 lbs or 10% of my body weight over the past 2-3 months and feel much better, but the severe palpitations do occur still without much warning. Last night I had an episode that lasted close to an hour and a half. After the palpitations reside and normal heart function returns, stomach sour sets in and I end up urinating frequently and also evacuating my bowells which help with recovery. My cardiologist says that the stomach sour is a result of the palpitations and not the other way around. My stomach isn't causing my palpitations. I will never take another med again in my life. It's poison to my system. How other's can tolerate this stuff is beyond me. I eat right and exercise everyday.

 Death

We have used the statistics obtained from the eHealthme web site compiled from Adverse Drug Reports submitted by doctors to the FDA and SEDA.  These figures thus include only those submitted by doctors as known adverse effects and only apply to the USA and not the rest of the world. 

  • On Jan, 15, 2016: 80,182 people reported to have side effects when taking Atenolol. Among them, 1,249 people (1.56%) have Death
  • On Jan, 28, 2016: 524 people reported to have side effects when taking Atenolol and chlorthalidone. Among them, 4 people (0.76%) have Death
  • On Jan, 17, 2016: 1,953 people reported to have side effects when taking Betapace. Among them, 39 people (2.00%) have Death
  • On Jan, 28, 2016: 116 people reported to have side effects when taking Betapace af. Among them, 2 people (1.72%) have Death
  • On Jan, 24, 2016: 15,619 people reported to have side effects when taking Bisoprolol fumarate. Among them, 285 people (1.82%) have Death
  • On Jan, 28, 2016: 795 people reported to have side effects when taking Bisoprolol fumarate and hydrochlorothiazide. Among them, 9 people (1.13%) have Death.
  • On Jan, 4, 2016: 161 people reported to have side effects when taking Brevibloc. Among them, 8 people (4.97%) have Death.
  • On Jan, 16, 2016: 19,044 people reported to have side effects when taking Carvedilol. Among them, 465 people (2.44%) have Death
  • On Jan, 4, 2016: 23,221 people reported to have side effects when taking Coreg. Among them, 868 people (3.74%) have Death
  • On Jan, 28, 2016: 2,063 people reported to have side effects when taking Corgard. Among them, 20 people (0.97%) have Death.
  • On Jan, 26, 2016: 9,302 people reported to have side effects when taking Inderal. Among them, 114 people (1.23%) have Death
  • On Jan, 2, 2016: 1,312 people reported to have side effects when taking Inderal la. Among them, 18 people (1.37%) have Death
  • On Jan, 2, 2016: 732 people reported to have side effects when taking Labetalol hydrochloride. Among them, 5 people (0.68%) have Death
  • On Jan, 2, 2016: 18,056 people reported to have side effects when taking Lopressor. Among them, 554 people (3.07%) have Death
  • On Jan, 24, 2016: 17,441 people reported to have side effects when taking Metoprolol succinate. Among them, 404 people (2.32%) have Death
  • On Jan, 8, 2016: 38,610 people reported to have side effects when taking Metoprolol tartrate. Among them, 970 people (2.51%) have Death
  • On Jan, 28, 2016: 240 people reported to have side effects when taking Metoprolol tartrate and hydrochlorothiazide. Among them, 7 people (2.92%) have Death
  • On Jan, 11, 2016: 1,824 people reported to have side effects when taking Nadolol. Among them, 32 people (1.75%) have Death.
  • On Jan, 1, 2016: 578 people reported to have side effects when taking Normodyne. Among them, 16 people (2.77%) have Death
  • On Jan, 21, 2016: 161 people reported to have side effects when taking Ocupress. Among them, 4 people (2.48%) have Death
  • On Jan, 3, 2016: 2,573 people reported to have side effects when taking Propranolol hydrochloride. Among them, 41 people (1.59%) have Death
  • On Jan, 11, 2016: 2,320 people reported to have side effects when taking Sectral. Among them, 26 people (1.12%) have Death
  • On Jan, 15, 2016: 1,941 people reported to have side effects when taking Sotalol hydrochloride. Among them, 23 people (1.18%) have Death
  • On Jan, 24, 2016: 14,191 people reported to have side effects when taking Tenormin. Among them, 324 people (2.28%) have Death
  • On Jan, 28, 2016: 3,652 people reported to have side effects when taking Timolol maleate. Among them, 69 people (1.89%) have Death
  • On Jan, 26, 2016: 39,663 people reported to have side effects when taking Toprol-xl. Among them, 830 people (2.09%) have Death
  • On Jan, 28, 2016: 963 people reported to have side effects when taking Zebeta. Among them, 17 people (1.77%) have Death

Deaths and Side effect total

If we now total the numbers above obtained from the eHealthme web site and compiled from Adverse Drug Reports submitted by doctors to the FDA and SEDA, where the figures thus include only those submitted by doctors as known adverse effects and only apply to the USA and not the rest of the world, we obtain the following totals:

Side effects 297, 137

Deaths 5,402

as at January 2016.  These are people affected, not incidences. 

How it works

I think one principle reason that people experience hallucinations, out of body and near death experiences from beta blockers is from the Bradycardia -  a slow heart beat. As explained above, Beta blockers aim to put less strain on the heart, but the problem is that bradycardia can result in fatigue, weakness, dizziness, and at very low rates fainting, in essence the bradycardia is causing hypoxia.

What has also emerged from the observations, however, is that beta blockers act almost like anaesthetics, in that they can cross the blood brain barrier.  Depending on their lipophilic state they then attack the various organs of the brain and cause general disruption.  This is perhaps better understood if you turn to the section on Inhaling volatiles and gases as in this context that is what the drugs are acting as.  There are some treatments that actually require the person to 'snort' the drug and the nose is a highly vulnerable site when it comes to any drug.  It is a mechanism of by passing the blood brain barrier entirely.

 

Over the years, beta-blockers have been associated with an incidence,…of CNS side effects. The question of interest, however, is whether the incidence is the same for all members of the class or whether other properties, such as hydrophilicity, have a bearing on the incidence of this type of side effect. … In pharmacokinetic terms the lipophilic beta-blockers have been shown, both in animals and man, to readily cross the blood-brain barrier in contrast to hydrophilic beta-blockers. This is thought to have possible clinical relevance with respect to the relative incidence of CNS side-effects. To clarify the situation every published clinical paper, in which the beta-blockers propranolol (highly lipophilic), pindolol (moderately lipophilic), metoprolol (moderately lipophilic) and atenolol (hydrophilic) were compared, was assessed for information pertaining to CNS side effects. This comprehensive review of …CNS side effects such as sleep disturbances, dreaming, nightmares and hallucinations following clinically accepted doses [shows that]the incidence of these side effects is lowest with hydrophilic atenolol and generally highest with pindolol and propranolol. Metoprolol occupies an intermediate position.  PMID:  1969642

 and

Beta-adrenoceptor blocking drugs can be characterised by their pharmacokinetic properties. One of the most important factors appears to be lipid solubility. Lipophilic beta-adrenoceptor antagonists, such as propranolol, oxprenolol and metoprolol, are cleared by the liver and undergo hepatic 'first-pass' metabolism. This results in low bioavailability, substantial interpatient variability in 'steady-state' plasma drug concentrations, rapid elimination half-lives and the possibility of drug interactions with other drugs such as pentobarbitone and cimetidine which affect hepatic enzymes. In addition, lipid soluble drugs are distributed widely within the body and penetrate the brain easily and rapidly. This may result in centrally mediated adverse effects such as vivid dreams. In contrast, the more water-soluble beta-adrenoceptor blocking drugs, such as atenolol, sotalol and nadolol, are cleared by the kidney unchanged. They show less interpatient variation in plasma levels, have longer elimination half-lives and do not interact with drugs affecting hepatic enzymes. They penetrate the central nervous system less easily and cause less central side-effect. Between these two extremes, there are several drugs like betaxolol, bisoprolol and pindolol, which are cleared partly by the liver and partly by the kidney. Their clearance is only altered by severe renal or hepatic disease, and they do not appear to interact with enzyme inducers or inhibitors.  PMID:  2897304

 

References and further reading

  • Hypertension. 1988 Mar;11(3 Pt 2):II21-9. Beta-adrenergic receptor blockers. Adverse effects and drug interactions.- Frishman WH.   Department of Medicine, Albert Einstein College of Medicine, Bronx, New York
  • Endocr Metab Immune Disord Drug Targets. 2013 Mar;13(1):125-34.  Managing erectile dysfunction in heart failure.  Giagulli VA1, Moghetti P, Kaufman JM, Guastamacchia E, Iacoviello M, Triggiani V.  1O.U. Metabolic Disease and Endocrinology, P.O. Conversano, Via De Amicis, 3070014 Conversano-Ba, Italy. vitogiagulli@alice.it
  • Visual hallucinations and metoprolol. - Sirois FJ. Psychosomatics. 2006 Nov-Dec;47(6):537-8.  PMID:  17116960
  • [Diabetic with hallucination].  Saloranta C, Tuomi T.  Duodecim. 2005;121(21):2319-20. Finnish. PMID:  16457114
  • Drug-induced musical hallucinations.  Gordon AG.  J Nerv Ment Dis. 1998 Oct;186(10):652-3. No abstract available.   PMID: 9788643
  • Musical hallucinations induced by propranolol.  Fernandez A, Crowther TR, Vieweg WV. J Nerv Ment Dis. 1998 Mar;186(3):192-4. No abstract available.   PMID: 9521357
  • [Adverse effects of atenolol on the central nervous system].  Galicia Basart MA, Rodríguez Jornet A, Maté Benito G, Herranz del Rey S.  Med Clin (Barc). 1988 Feb 27;90(8):353. Spanish. No abstract available.   PMID:  3374196
  •  [Visual hallucinations induced by pindolol].  Pines A, Goldhammer E, Frankl O.  Harefuah. 1983 Mar 15;104(6):226-7. Hebrew. PMID:  6618310
  • Central nervous system side effects of propranolol.  Tikare SK, Bandisode MS.  J Med Assoc Ga. 1982 Nov;71(11):777-8.  PMID:  7175387
  • Propranolol-induced hallucinosis.  Horn JR, Rylander ML, Hicks HM.  Clin Pharm. 1982 Sep-Oct;1(5):464-8. PMID:  7184681
  • Propranolol and white rabbits.  White WB, Riotte K.  N Engl J Med. 1982 Aug 26;307(9):558-9. PMID:  7099233
  • Propranolol psychosis.  Whitlock FA, Bonfield AR.  Med J Aust. 1980 Feb 23;1(4):184-5 PMID:  7374553
  •  [Hallucinations after taking pindolol (author's transl)].  Rodor F, Poyen B, Santoni Y, Thomas JL, Ripert JL, Jouglard J.  Nouv Presse Med. 1979 Jun 30;8(29):2417-8. French. No abstract available.   PMID:  493028
  • Prolonged delirium with propanolol.  Kuhr BM.  J Clin Psychiatry. 1979 Apr;40(4):198-9.  PMID:  33971
  • Eur Heart J. 1987 Dec;8 Suppl M:9-14.  Comparison of pharmacokinetic properties of beta-adrenoceptor blocking drugs.  McDevitt DG.  Department of Pharmacology and Clinical Pharmacology, Ninewells Hospital, Dundee, U.K.
  • J Allergy Clin Immunol. 2015 Feb;135(2):491-9. doi: 10.1016/j.jaci.2014.09.004. Epub 2014 Oct 16.  Ramipril and metoprolol intake aggravate human and murine anaphylaxis: evidence for direct mast cell priming.  Nassiri M1, Babina M1, Dölle S1, Edenharter G2, Ruëff F3, Worm M4.
 

Observations

The table blow shows in summary form the number of hallucinations for the drugs, the links take you to the eHealthme website and the page for side-effects in general for each drug.  If these links do not work, it may be because eHealthme are busy revising the figures, or because the drug has been renamed, or because it has been withdrawn.  These figures were collected in 2010.  The observations contain more recent figures.  Please note the objective is to provide an indication, as the figures will only every be a snapshot.

Observation no

Drug Name

No of hallucinations

 

Acebutolol  trade names Sectral and Prent

20

005085

Atenolol

180

005085

Tenormin

176

005086

Bisoprolol

52

005086

Zebeta

39

005087

Coreg

60

005087

Carvedilol

58

005088

Metoprolol

481

005088

Lopressor

103

005088

Toprol-xl

186

005089

Propranolol

74

005089

Inderal

188

005090

Sotalol

24

012263

Nadolol

17

 012271

Timolol

40

 

 

1,698

Related observations